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10-000-MPPT

Matched Pair Tissue Slides - Breast Tissue

The Matched Pair Paraffin Tissue (MPPT) slides are designed for identifying tumor-specific/metastasis genes or proteins. Slices from normal and malignant tissues are mounted on each MPPT slide which can then be treated as a single histological slide for H&E staining, immunohistochemistry, or in situ hybridization. This format allows a rapid analysis of protein expression and localization across normal and cancerous tissue.

497.63 €

10-001-10um

Breast Tissue Slide (Normal)

497.63 €

10-001-4um

Breast Tissue Slide (Normal)

459.45 €

10-002

SARS-CoV-2 (COVID-19) ORF8 Recombinant Protein

LOCUS: QHD43422 121aa linear VRL 18-MAR-2020 DEFINITION: ORF8 protein [Severe acute respiratory syndrome coronavirus 2] ACCESSION: QHD43422 VERSION:QHD43422.1 DBSOURCE: accession MN908947.3 SOURCE: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ORGANISM: Viruses, Riboviria, Nidovirales, Cornidovirineae, Coronaviridae,Orthocoronavirinae, Betacoronavirus, Sarbecovirus.LOCUS: QHD43422 121aa linear VRL 18-MAR-2020 DEFINITION: ORF8 protein [Severe acute respiratory syndrome coronavirus 2] ACCESSION: QHD43422 VERSION:QHD43422.1 DBSOURCE: accession MN908947.3 SOURCE: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ORGANISM: Viruses, Riboviria, Nidovirales, Cornidovirineae, Coronaviridae,Orthocoronavirinae, Betacoronavirus, Sarbecovirus.LOCUS: QHD43422 121aa linear VRL 18-MAR-2020 DEFINITION: ORF8 protein [Severe acute respiratory syndrome coronavirus 2] ACCESSION: QHD43422 VERSION:QHD43422.1 DBSOURCE: accession MN908947.3 SOURCE: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ORGANISM: Viruses, Riboviria, Nidovirales, Cornidovirineae, Coronaviridae,Orthocoronavirinae, Betacoronavirus, Sarbecovirus.

1213.46 €

10-004-10um

Breast Tissue Slide (Fibroadenoma)

497.63 €

10-004-4um

Breast Tissue Slide (Fibroadenoma)

459.45 €

10-005

SARS-CoV-2 (COVID-19) ORF3a Recombinant Protein

LOCUS: QHD43417 275aa linear VRL 18-MAR-2020 DEFINITION: ORF3a protein [Severe acute respiratory syndrome coronavirus 2] ACCESSION: QHD43417 VERSION:QHD43417.1 DBSOURCE: accession MN908947.3 SOURCE: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ORGANISM: Viruses, Riboviria, Nidovirales, Cornidovirineae, Coronaviridae,Orthocoronavirinae, Betacoronavirus, Sarbecovirus.

1213.46 €

10-008

SARS-CoV-2 (COVID-19) Spike-RBD Recombinant Protein

SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2) also known as 2019-nCoV (2019 Novel Coronavirus) is a virus that causes illnesses ranging from the common cold to severe diseases. SARS CoV-2 spike protein is composed of S1 domain and S2 domain. S1 contains a receptor-binding domain (RBD) that can specifically bind to angiotensin-converting enzyme 2 (ACE2), the receptor on the target cells. SARS-CoV-2 spike protein (RBD) has the potential value for the diagnosis of the virus.

1213.46 €

10-009-10um

Breast Tissue Slide (Invasive Mammary Carcinoma)

497.63 €

10-009-4um

Breast Tissue Slide (Invasive Mammary Carcinoma)

459.45 €

10-010-10um

Breast Tissue Slide (Ductal Carcinoma In Situ (DCIS))

497.63 €

10-010-4um

Breast Tissue Slide (Ductal Carcinoma In Situ (DCIS))

459.45 €

10-012-10um

Breast Tissue Slide (Well Differentiated Carcinoma)

497.63 €

10-012-4um

Breast Tissue Slide (Well Differentiated Carcinoma)

459.45 €

10-013-10um

Breast Tissue Slide (Poorly Differentiated Carcinoma)

497.63 €

10-013-4um

Breast Tissue Slide (Poorly Differentiated Carcinoma)

459.45 €

10-014

ACE-2 Recombinant Protein

Angiotensin-Converting Enzyme 2 (ACE-2) is an integral membrane protein and a zinc metalloprotease of the ACE family which includes somatic and germinal ACE. ACE-2 cleaves angiotensins I and II as a carboxypeptidase and converts angiotensin I to angiotensin 1-9, and angiotensin II to angiotensin 1-7. ACE-2 is also able to hydrolyze apelin-13 and dynorphin-13 with high efficiency. ACE-2 can be highly expressed in testis, kidney, heart, colon, small intestine and ovary at moderate levels. ACE2 is not inhibited by the classical ACE inhibitors, captopril and lisinopril and may play an important role in regulating the heart function.

1213.46 €

10-015

SARS-CoV-2 (COVID-19) Spike-RBD Recombinant Protein

1213.46 €

10-016

Amastatin . hydrochloride

Slow, tight binding and competitive aminopeptidase (AP) inhibitor. Inhibits cytosolic leucine aminopeptidase, microsomal aminopeptidase M and bacterial leucine aminopeptidase, human serum aminopeptidase A (AP-A), aminopeptidase N (AP-N), tyrosine aminopeptidase, but not aminopeptidase B (AP-B). Amastatin is without effect on trypsin, papain, chymotrypsin, elastase, pepsin or thermolysin. Inhibits completely the Suc-Ala-Ala-Pro-Leu-pNA amidolytic enzyme. Slightly inhibits the formation of angiotensin III (Ang III) from Angiotensin II through AP-A, but significantly increases the potency of angiotensin III and [des-Asp1]-angiotensin I. Moderate inhibitor of mitochondrial intermediate peptidase (MIP). Weak inhibitor of simian immunodeficiency virus protease (SIV-PR). ANPEP (aminopeptidase N) is a host receptor targeted by porcine epidemic diarrhoea virus, human coronavirus 229E, feline coronavirus, canine coronavirus, transmissible gastroenteritis virus and infectious bronchitis virus. These viruses all belong to coronaviridae. ANPEP is therefore investigated as a potential target for SARS-CoV-2 infections.

799.23 €

10-017

Camostat . mesylate

Camostat is an orally bioavailable trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein and thrombin. Camostat has been shown to inhibit the production of TNF-Î± and monocyte chemoattractant protein-1 by monocytes and to disrupt proliferation of pancreatic stellate cells in a rat model of pancreatic fibrosis. Protease regulation via camostat has also been reported to reversibly inhibit epithelial sodium channel function in human airway epithelial cell models. It is used in the treatment of some forms of cancer and is also effective against some viral infections (such as SARS, MERS or influenza), as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It suppresses pancreatitis-induced pain in rats following oral administration and is used to treat pancreatitis and reflux esophagitis after gastrectomy. It is an inhibitor of the enzyme transmembrane serine protease TMPRSS2 and partially blocks infection by SARS-CoV and human coronavirus NL63 in HeLa cells and entry of SARS-CoV2 (COVID-19) into lung cells in vitro.

753.42 €

10-018

Chloroquine . diphosphate

Chloroquine is a commonly used antimalarial drug, more toxic than its derivative hydroxychloroquine (Prod. No. AG-CR1-3720). Chloroquine has anti-inflammatory, immunomodulating, anti-infective, antiviral, antithrombotic and metabolic effects. It has anticancer properties, related to their strong antiproliferative, antimutagenic, epigenetic and autophagy inhibiting and apoptosis inducing activities. Chloroquine is used to treat rheumatoid arthritis, systemic lupus erythematosus, antiphospholipid antibody syndrome and SjÃ¶gren's syndrome. Chloroquine interfers with lysosomal activity and autophagy, interacts with membrane stability and alters signaling pathways and transcriptional activity, which can result in inhibition of cytokine production and modulation of certain co-stimulatory molecules. Chloroquine shows antiviral activity against several viruses by inhibiting viral replication and inhibits SARS-CoV-2 viral infection (COVID-19) in vitro.

696.15 €

10-019

Hydroxychloroquine . sulfate

Hydroxychloroquine is a synthetic less toxic derivative of chloroquine (Prod. No. AG-CR1-3721), commonly used as an antimalarial drug. Hydroxychloroquine has anti-inflammatory, immunomodulating, anti-infective, antiviral, antithrombotic and metabolic effects. It has anticancer properties, related to their strong antiproliferative, antimutagenic, epigenetic and autophagy inhibiting and apoptosis inducing activities. Hydroxychloroquine is used to treat rheumatoid arthritis, systemic lupus erythematosus, antiphospholipid antibody syndrome and SjÃ¶gren's syndrome. Hydroxychloroquine interfers with lysosomal activity and autophagy, interacts with membrane stability and alters signaling pathways and transcriptional activity, which can result in inhibition of cytokine production and modulation of certain co-stimulatory molecules. It increases lysosomal pH in antigen-presenting cells and blocks in inflammatory conditions, toll-like receptors on plasmacytoid dendritic cells (PDCs). By decreasing TLR signaling, it reduces the activation of dendritic cells and the inflammatory process. It also acts as an antagonist TLR7 and TLR9. Hydroxychloroquine shows antiviral activity against several viruses by inhibiting viral replication and inhibits SARS-CoV-2 viral infection (COVID-19), in vitro.

753.42 €

10-020-10um

Breast Tissue Slide (Abnormal)

497.63 €

10-020-4um

Breast Tissue Slide (Abnormal)

459.45 €

10-021

Darunavir

Darunavir is a highly potent HIV protease inhibitor (IC50=3-6nM, depending on laboratory HIV-1 strain), an antiretroviral medication used to treat and prevent HIV/AIDS. Darunavir is a second generation HIV-1 protease inhibitor that inhibits replication of various laboratory strains and clinical isolates of HIV-1, including those resistant to first generation protease inhibitors. It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations. Formulations containing darunavir have been used in combination therapy for the treatment of HIV. The Darunavir ethanolate (Prod. No. AG-CR1-3724) formulation has some stability advantages compared to the free base Darunavir. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the papain-like viral protease (PLVP) of SARS-CoV-2, responsible for COVID-19.

890.86 €

10-022

Darunavir . ethanolate

Darunavir ethanolate is a highly potent HIV protease inhibitor (IC50=3-6nM, depending on laboratory HIV-1 strain), an antiretroviral medication used to treat and prevent HIV/AIDS. The ethanolate formulation has some stability advantages compared to the free base Darunavir (Prod. No. AG-CR1-3712). Darunavir ethanolate is a second generation HIV-1 protease inhibitor that inhibits replication of various laboratory strains and clinical isolates of HIV-1, including those resistant to first generation protease inhibitors. It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations. Formulations containing darunavir have been used in combination therapy for the treatment of HIV. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the papain like viral protease (PLVP) of SARS-CoV-2, responsible for COVID-19.

845.05 €

10-023

Ebselen

Glutathione peroxidase mimetic [1, 4]. Peroxynitrite scavenger [4]. Anti-inflammatory [1, 5-7] Antioxidant [2, 3, 5]. Protein kinase C (PKC), NADPH, lipoxygenase, COX, NOS, H+-ATPase and NADPH oxidase inhibitor [6-9]. Antifungal [9]. Review [10]. Potent IDO-1 inhibitor with Ki 94nM [11]. Inhibitor of HIV-1 capsid C-terminal domain dimerization. Shown to potentially inhibit the 33.8-kDa Main Protease (Mpro)/3C-like Protease of SARS-CoV-2, consequently inhibiting viral transcription and replication and possibly inhibiting spread of COVID-19

661.79 €

10-024

EIDD-2801

EIDD-2801 is an orally bioavailable prodrug of the antiviral nucleoside derivative N4-hydroxycytidine (NHC, EIDD-1931). It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase. It exerts its antiviral action through introduction of copying errors during viral RNA replication. The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe. The broad-spectrum antiviral agent EIDD-2801 inhibits viral RNA replication in various unrelated RNA viruses including influenza, Ebola, Venezuelan equine encephalitis virus (VEEV) and coronaviruses, including SARS-CoV, MERS-CoV and SARS-CoV-2. EIDD-2801 has the potential for COVID-19, seasonal and pandemic influenza treatment.

799.23 €

10-025

Elbasvir

Elbasvir is a direct-acting antiviral drug that potently inhibits hepatitis C virus (HCV) non-structural protein 5A (NS5A). NS5A is essential for HCV RNA synthesis and viral assembly, and elbasvir inhibits the assembly of new viral replicase complexes when used at a concentration of 50 pM. It exhibits potent inhibitory activity against a broad range of HCV genotypes. Formulations containing elbasvir have been used alone and in combination with NS3/4A protease inhibitors in the treatment of HCV. Identified as a potential inhibitor of SARS-CoV-2, responsible for COVID-19.

764.87 €

10-026

Famotidine

Famotidine is a histamine H2 receptor antagonist. It is selective for H2 over H1 and muscarinic receptors (Kis = 4 and 28 ÂµM, respectively, in bovine cerebral cortex). Famotidine blocks the action of histamine in the parietal cells, ultimately blocking acid secretion in the stomach. It inhibits histamine-induced acid secretion in isolated canine parietal cells (IC50 = 0.6ÂµM) and suppresses histamine-induced gastric acid secretion in dogs when administered orally and in anesthetized rats when administered intraduodenally (ID50s = 10 and 400Âµg/kg, respectively). Famotidine is used to treat ulcers, gastroesophageal reflux disease (GERD) and heartburn and it decreases the risk of gastrointestinal toxicity associated with non-steroidal anti-inflammatory drugs (NSAIDs). Potential inhibitor of the viral enzyme papain-like protease (PLpro), important for SARS-CoV-2 replication and being tested in COVID-19 clinical trials.

719.06 €

10-027

Favipiravir

The guanine analog Favipiravir is a broad spectrum inhibitor of viral RNA polymerase, acting on viral genetic copying to prevent its reproduction. Favipiravir is a prodrug that is metabolized to its active form, favipiravir-ribofuranosyl-5'-triphosphate (Favipiravir-RTP), which inhibits selectively RNA-dependent RNA polymerase (RdRp) in RNA viruses. This antiviral agent inhibits influenza A, B and C without inducing cytotoxicity up to 1,000 Âµg/ml. It also inhibits influenza strains resistant to current antiviral drugs and shows a synergistic effect in combination with oseltamivir (Prod. No. AG-CR1-3714), thereby expanding influenza treatment options. Favipiravir is active against a variety of additional viruses, including West Nile virus, yellow fever virus, foot-and-mouth disease virus as well as other flaviviruses, arenaviruses, bunyaviruses and alphaviruses in vitro and in vivo. Activity has also been shown against enteroviruses, Rift Valley fever virus and Marburg virus (MARV9), while limited efficacy has been shown against Ebola virus (EBOV) and Zika virus in animal studies. Favipiravir shows potential efficacy against SARS-CoV-2 and is undergoing clinical studies to test its efficacy and safety in the treatment of coronavirus disease 2019 (COVID-19).

799.23 €

10-028

Imatinib . mesylate

Imatinib mesylate is a multitarget tyrosine kinase inhibitor with antineoplastic activity. It is a potent and selective inhibitor of the kinases Bcr-Abl (IC50 = 38 nM), PDGFR and c-Kit, which are encoded by the bcr-abl oncogene as well as receptor tyrosine kinases encoded by c-Kit and platelet-derived growth factor receptor (PDGFR) oncogenes, which is useful in vitro and in vivo. Imatinib inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit and the proliferation of Bcr-Abl-dependent R10 cells and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner. Formulations containing imatinib have been used in the treatment of various cancers. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis and myelodysplastic syndrome. Abelson (Abl) kinase inhibitors have been shown to inhibit replication of Ebola virus, coxsackievirus and vaccinia virus, but at different points of the virus life cycle. Imatinib inhibits replication of SARS-CoV and MERS-CoV in vitro by a novel mechanism of blocking coronavirus virion fusion with the endosomal membrane. Abl is also a potential drug target of SARS-CoV-2 and can possible inhibit the spread of COVID-19.

845.05 €

10-029

Lopinavir

The antiviral agent Lopinavir is a potent inhibitor of HIV-1 protease (Ki=1.3pM for wild-type enzyme) and has been shown to block the replication of clinical isolates of HIV (EC50s=5-52nM). Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir). Lopinavir/ritonavir inhibits the HIV protease enzyme by forming an inhibitor-enzyme complex thereby preventing cleavage of the gag-pol polyproteins. Immature, non- infectious viral particles are subsequently produced. Lopinavir also has an ability to inhibit ZMPSTE24 (zinc metallopeptidase STE24). HIV-PIs block prelamin A processing by directly affecting the enzymatic activity of ZMPSTE24 and in this way they may contribute to lipodystrophy in individuals undergoing HIV-PI treatment. It also has been shown to inhibit meningioma cell proliferation, induce apoptosis on lymphoma cells and inhibit insulin signaling. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the coronavirus endopeptidase C30 (CEP_C30) of SARS-CoV-2. A initial randomized trial study was not successful.

833.59 €

10-030

Mycophenolic acid

Antibiotic [1]. Shows antiviral, antifungal and antitumor properties [1, 2]. Immunosuppressive drug used to prevent rejection in organ transplantation, rheumatoid arthritis, and psoriasis [3-6, 13]. Potent reversible inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH), leading to depletion of GMP and interruption of the de novo synthesis of purine nucleotides necessary for B and T lymphocyte proliferation [7, 8]. Inhibits the type II IMPDH isoform (IMPDH-2) 5-fold more potently compared to type I isoform [11]. Inhibits RNA and DNA synthesis [13]. Inducible nitric oxide synthase (iNOS/NOS II) inhibitor [8, 10]. Apoptosis and necrosis inducer [9, 12]. Novel type of inhibitor against RNA guanylyltransferases [14]. Inhibits TNF-Î±-stimulated MAPK/NF-ÎºB and ROS generation [15]. Autophagy suppressor. Broad-spectrum antiviral compound with inhibitory activity against different coronavirus, including SARS-CoV, MERS-CoV and SARS-CoV-2, cause of COVID-19. It binds to the active site of SARS-CoV-2 papain-like protease (PLpro) possibly inhibiting viral replication.

948.13 €

10-031

Nafamostat . mesylate

Nafamostat mesylate is a cell permeable broad spectrum potent and reversible synthetic serine protease inhibitor and kallikrein inhibitor in vitro and in vivo. It inhibits trypsin (Ki=15nM), tryptase (Ki=95.3pM) and additional proteases in the coagulation cascade including thrombin (Ki=0.84ÂµM). Nafamostat mesylate is a short-acting anticoagulant with anti-inflammatory, anticancer and antiviral properties. As a potential anticancer agent, it blocks canonical NF-ÎºB signaling, targets TNFR1-stimulated cleavage of caspase families and the tryptase of mast cells to improve therapeutic outcome and to ameliorate cancer therapy resistance and avoid immune resistance. It has been shown to reduce eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. Inhibits the demethylase activity of the fat mass and obesity-associated protein (FTO). As antiviral agent, it inhibits Ebola virus, MERS-CoV and SARS-CoV-2 infection in vitro and potentially the spread of COVID-19. Nafamostat mesylate inhibits TMPRSS2-dependent host cell entry of MERS-CoV. It is also an inhibitor of the enzyme transmembrane serine protease TMPRSS2 and blocks the entry of SARS-CoV-2 (COVID-19) into lung cells in vitro, with roughly 15-fold higher efficiency than Camostat mesylate (Prod. No. AG-CR1-3716), with an EC50 in the low nanomolar range.

799.23 €

10-032

Nelfinavir . mesylate

Nelfinavir is an orally bioavailable competitive inhibitor of the human immunodeficiency virus. It potently inhibits HIV-1 (Ki=2nM) and HIV-2 protease in vitro. HIV-1 protease is important for the replication of the virus within the cell and the release of mature viral particles from the infected cell. Formulations containing nelfinavir have been used in combination with HIV reverse transcriptase inhibitors for the treatment of AIDS. Nelfinavir shows other antimicrobial and antiviral activity. It inhibits maturation and export of the Herpes Simplex 1 virus and the Kaposi's Sarcoma virus, replication of SARS-CoV and also replication of SARS-CoV-2, cause for the epidemic COVID-19. Has potent anti-cancer activity against a broad selection fo cancer cell types. Shown to induce apoptosis, autophagy, cell cycle arrest and endoplasmic reticulum stress, which consequently leads to cancer cell death. Shown to inhibit the Akt/PKB signaling pathway. It acts as an antifibrotic agent and is used to treat pulmonary fibrosis in patients with systemic sclerosis (SSc) and reduces inflammation by activating protein phosphatase 2 (PP-2) and blocking mitogen-activated protein kinases (MAPK) signaling in macrophages.

867.95 €

10-033

Niclosamide

Antihelminthic, molluscicide and trypanocidal agent that inhibits mitochondrial oxidative phosphorylation and anaerobic ATP production. Anticancer agent with antiproliferative activity in a broad spectrum of cancer cells. Targets and inhibits multiple signaling pathways, including STAT3, NF-kB, Wnt/Î²-catenin, Notch and mTORC1. Shown to block TNF-Î±-induced IÎºBÎ± phosphorylation, translocation of p65 and the expression of NF-ÎºB-regulated genes and elevates reactive oxygen species (ROS) levels. Promotes Frizzled1 internalization, down-regulates the expression of Dishevelled-2 protein and inhibits Î²-catenin stabilization. Inhibits mTORC1 but not mTORC2 signaling in cells maintained in nutrient-rich conditions. Cell permeable selective STAT3 inhibitor (IC50=0.25Î¼M). Inhibits the activation, nuclear translocation and transactivation of STAT3. Selective over STAT1, STAT5, JAK1, JAK2 and Src kinases. Induces cell cycle arrest, growth inhibition, autophagy and apoptosis. Inhibits S100A4 (Metastasin-1)-induced metastasis in vivo. Inhibits androgen receptor (AR) splice variants. Anti-inflammatory compound. Quorum sensing inhibitor. Broad-spectrum antiviral agent that targets acidified endosomes. Has been shown to inhibit replication of SARS and is a potential candidate to treat SARS-CoV-2 (COVID-19) infections. Antiobesity and antidiabetic agent. Positive allosteric neuropetide Y4 receptor ligand and increases energy expenditure and lipid metabolism through mitochondrial uncoupling.

719.06 €

10-034

Niclosamide . ethanolamine

With slightly better solubility properties compared to Niclosamide (Prod. No. AG-CR1-3643). Antihelminthic, molluscicide and trypanocidal agent that inhibits mitochondrial oxidative phosphorylation and anaerobic ATP production. Anticancer agent with antiproliferative activity in a broad spectrum of cancer cells. Targets and inhibits multiple signaling pathways, including STAT3, NF-kB, Wnt/Î²-catenin, Notch and mTORC1. Shown to block TNF-Î±-induced IÎºBÎ± phosphorylation, translocation of p65 and the expression of NF-ÎºB-regulated genes and elevates reactive oxygen species (ROS) levels. Promotes Frizzled1 internalization, down-regulates the expression of Dishevelled-2 protein and inhibits Î²-catenin stabilization. Inhibits mTORC1 but not mTORC2 signaling in cells maintained in nutrient-rich conditions. Cell permeable selective STAT3 inhibitor (IC50=0.25Î¼M). Inhibits the activation, nuclear translocation and transactivation of STAT3. Selective over STAT1, STAT5, JAK1, JAK2 and Src kinases. Induces cell cycle arrest, growth inhibition, autophagy and apoptosis. Inhibits S100A4 (Metastasin-1)-induced metastasis in vivo. Inhibits androgen receptor (AR) splice variants. Anti-inflammatory compound. Quorum sensing inhibitor. Broad-spectrum antiviral agent that targets acidified endosomes. Has been shown to inhibit replication of SARS and is a potential candidate to treat SARS-CoV-2 (COVID-19) infections. Antiobesity and antidiabetic agent. Positive allosteric neuropetide Y4 receptor ligand and increases energy expenditure and lipid metabolism through mitochondrial uncoupling.

776.33 €

10-035

Nitazoxanide

Nitazoxanide is a broad-spectrum antiparasitic, antimicrobial and antiviral drug that is used in medicine for the treatment of various helminthic, protozoal, bacterial and viral infections. Nitazoxanide is rapidly metabolized to tizaxonide, an antiparasitic drug of the thiazolide class. The anti-protozoal activity and activity against anaerobic bacteria is believed to be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic energy metabolism. Nitazoxanide also showed a variety of other antibacterial mechanisms, inhibiting pyruvate dehydrogenase in E. coli, disrupting the membrane potential and pH homeostasis in the Mycobacterium tuberculosis and suppressing the chaperone/usher (CU) pathway of the Gram-negative bacteria. It is being studied for potential treatment for chronic hepatitis B, chronic hepatitis C, rotavirus, norovirus gastroenteritis and the coronavirus SARS-CoV-2 (COVID-19). The mechanism is suppressing the viral replication by inhibiting maturation of the viral hemagglutinin and the viral transcription factor immediate early 2 (IE2) as well as by activating the eukaryotic translation initiation factor 2Î± (an antiviral intracellular protein). Nitazoxanide modulates a variety of other pathways in vitro, including glutathione-S-transferase and glutamate-gated chloride ion channels in nematodes, respiration and other pathways in bacteria and cancer cells and viral and host transcriptional factors. Nitazoxanide has also been shown to be a potent antagonist of the Ca2+-activated Cl- channel TMEM16A, which offers a new mechanism to bronchodilate airways and block the multiple contractiles operating in severe diseases.

902.31 €

10-036

Oseltamivir . phosphate

Oseltamivir phosphate is an influenza viral neuraminidase inhibitor. It is an antiviral prodrug targeted against the influenza viruses. Once hydrolyzed in the liver to its active metabolite, oseltamivir carboxylate, it can competitively inhibit viral neuraminidase (IC50s=0.1-4.9nM for influenza neuraminidases A and B). The enzyme cleaves the sialic acid which is found on glycoproteins on the surface of human cells that helps new virions to exit the cell. Thus oseltamivir is blocking the release of new viral particles from a host cell. Oseltamivir phosphate is used clinically to treat influenza A and influenza B and to prevent flu after exposure. It potentially could be used to reduce the spread of the SARS-CoV-2 and counteract against the transmission of COVID-19

719.06 €

10-037

Remdesivir

Remdesivir is an adenosine triphosphate analog with broad-spectrum antiviral activity. It is a prodrug that metabolizes into its active form GS-441524 (Prod. No. AG-CR1-3722). GS-441524 is an adenosine nucleotide analog in viral RNA production. It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase and evades proofreading by viral exoribonuclease (ExoN), causing a decrease in viral RNA production (RNA synthesis arrest), either by terminating RNA chains or causing mutations. It inhibits MERS-CoV or SARS-CoV-infected HAE cultures (EC50=74nM and 69nM) and murine hepatitis virus (MHV) (EC50=30nM). In vivo, remdesivir (25 and 50 mg/kg) reduces lung viral titers and prevents weight loss in a mouse model of SARS-CoV infection. Remdesivir is used as a treatment for Ebola virus disease and Marburg virus infections, and other single stranded RNA viruses such as respiratory syncytial virus, Junin virus, Lassa fever virus, Nipah virus, Hendra virus and the coronaviruses (including MERS and SARS viruses). Remdesivir is effective in the control of 2019-nCoV (COVID-19) infection in vitro. It now also has been studied as potential treatment of SARS-CoV-2 infections.

936.67 €

10-038

GS-441524 (Remdesivir Metabolite)

GS-441524 is the active prodrug of the broad-spectrum antiviral Remdesivir. GS-441524 is an adenosine nucleotide analog in viral RNA production. It is a nucleotide analog inhibitor of RNA-dependent RNA polymerases (RdRps). The compound interferes with the action of viral RNA polymerase and evades proofreading by viral exoribonuclease (ExoN), causing a decrease in viral RNA production (RNA synthesis arrest), either by terminating RNA chains or causing mutations. It inhibits MERS-CoV or SARS-CoV-infected HAE cultures (EC50=74nM and 69nM) and murine hepatitis virus (MHV) (EC50=30nM). In vivo, remdesivir (Prod. No. AG-CR1-3713) (25 and 50 mg/kg) reduces lung viral titers and prevents weight loss in a mouse model of SARS-CoV infection. Remdesivir (Prod. No. AG-CR1-3713) is used as a treatment for Ebola virus disease and Marburg virus infections and other single stranded RNA viruses such as respiratory syncytial virus, Junin virus, Lassa fever virus, Nipah virus, Hendra virus and the coronaviruses (including MERS and SARS viruses). Remdesivir is effective in the control of 2019-nCoV (COVID-19) infection in vitro. It now also has been studied as potential treatment of SARS-CoV-2 infections

890.86 €

10-039

Ribavirin

Ribavirin is a guanosine analog with broad-spectrum antiviral properties against DNA and RNA viruses, including coronavirus SARS, respiratory syncytial virus, several hemorrhagic fever viruses, hepatitis C (HCV) and influenza. It is also tested for SARS-CoV-2. It acts as a prodrug that can be activated by either mono- or tri-phosphorylation by cellular kinases. These phosphorylated derivatives of ribavirin have diverse effects on both cellular and viral enzymes, resulting in suppression of viral replication and propagation. There are 3 direct mechanisms of action, i) by inhibition of the viral RNA dependent RNA polymerase (RdRp) and RNA synthesis through direct interaction with ribavirin-5'-triphosphate, ii) by interfering with RNA capping activity, and iii) by increasing viral mutation rates through the misincorporation of RBV into the genome. In addition there are also 2 proposed indirect mechanisms, iv) inhibition of inosine monophosphate dehydrogenase (IMPDH) by ribavirin-5'-monophosphate, which leads to the depletion of intracellular GTP pools, v) unphosphorylated Ribavirin has immunomodulatory effects on antiviral cellular responses, enhancing the T-helper type 1 over type 2 responses or upregulating the interferon-stimulated response element. Ribavirin shows anticancer properties. The principal target in several cancers is the oncogenic eukaryotic translation initiation factor 4E (eIF4E), modulated via direct binding and competitive inhibition. Ribavirin has been shown to bind eIF4E at the functional site used to bind the m7G cap of mRNA transcripts in vitro. It competes with target mRNAs for binding, subsequent translocation to the cytoplasm and ultimately translation. Other studies also demonstrate modulation of several other key pathways including ERK, EZH2 and IMPDH.

707.61 €

10-040

Ritonavir

HIV-1 and HIV-2 protease inhibitor. Glucose transporter 1 (GLUT1) and 4 (GLUT4) inhibitor. Inhibits transport of glucose across the plasma membranes of mammalian cells and consequently decreases glycolysis. Useful agent for immunometabolism research. Antitumor agent. Apoptosis inducer and cell proliferation inhibitor in GLUT1/GLUT4 overexpressed cancer cell lines. Tumor cells rely on elevated glucose consumption and metabolism for survival and proliferation. Glucose transporters mediating glucose entry are key proximal rate-limiting checkpoints. Among the fourteen SLC2A family members, GLUTs 1 and 4 are high-affinity glucose transporters. The proteinase inhibitor Kaletra, which is a mixture of the HIV-1 proteinase inhibitors lopinavir and ritonavir has been shown to be effective against SARS-CoV and MERS-CoV. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the coronavirus endopeptidase C30 (CEP_C30) of SARS-CoV-2. An initial randomized trial study was not successful.

741.97 €

10-041

Rosuvastatin . calcium salt

Rosuvastatin is a potent competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in the cholesterol biosynthetic pathway and the target of the statin class of cholesterol-lowering drugs. Rosuvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease. Formulations containing rosuvastatin reduce low-density lipoprotein (LDL) and C-reactive protein and increase high-density lipoprotein (HDL) in humans. Shown to have anti-inflammatory, antioxidant, antithrombotic and insulin sensitizing properties. Identified as a potential inhibitor of SARS-CoV-2, responsible for COVID-19.

856.50 €

10-042

Ruxolitinib (free base)

Antineoplastic, anti-inflammatory and immunomodulating agent. Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM). Affects DC differentiation and function, leading to impaired T cell activation. Used in the treatment of myeloproliferative neoplasms and psoriasis. Anticancer agent. Shown to induce apoptosis and autophagy. Potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro. It is investigated against the spread of the SARS-CoV-2 (COVID-19).

764.87 €

10-043

Ruxolitinib . phosphate salt

Water-soluble phosphate salt of Ruxolitinib. Antineoplastic, anti-inflammatory and immunomodulating agent. Orally bioavailable potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5nM, respectively and is less selective for JAK3 (IC50=322nM). Affects DC differentiation and function, leading to impaired T cell activation. Used in the treatment of myeloproliferative neoplasms and psoriasis. Anticancer agent. Shown to induce apoptosis and autophagy. Potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro. It is investigated against the spread of the SARS-CoV-2 (COVID-19)

719.06 €

10-044

Saquinavir . mesylate

Saquinavir is an antiretroviral inhibitor of the human immunodeficiency virus. It potently inhibits HIV-1 (Ki=0.12nM) and HIV-2 (Ki<0.1nM) protease in vitro. HIV-1 protease is important for the replication of the virus within the cell and the release of mature viral particles from the infected cell. Formulations containing saquinavir have been used in combination with other inhibitors for the treatment of AIDS. Saquinavir shows other antimicrobial and antiviral activity. Potential SARS-CoV-2 replication inhibitor, responsible for COVID-19. Shows anti-cancer activity. Shown to induce apoptosis, autophagy and endoplasmic reticulum stress, which consequently leads to cancer cell death. Anti-inflammatory agent. Blocks cathepsin V and thereby inhibits disulfide HMGB1-induced TLR4 activation and cytokine production.

799.23 €

10-045

Shikonin

Anticancer compound. Inhibits TNF-Î±-induced and B-16 melanoma-induced angiogenesis. Induces apoptosis and RIP1- and RIP3-dependent necroptosis in several cancer cells. Circumvents cancer antidrug resistance through the necroptosis pathway. Proteasome inhibitor. Autophagy inducer. Topoisomerase I inhibitor. Inhibits glycolysis in cancer cells by inhibiting tumor-specific pyruvate kinase M2 (PKM2). Anti-inflammatory compound. Inhibits leukocyte migration, downregulates chemokine receptor expression, and inhibits HIV-1 replication. Inhibits the activation of NLRP3 and AIM2 inflammasome. Shown to directly target caspase-1 and as a inhibitor of PKM2 to block PKM2-mediated glycolysis that promotes inflammasome activation by modulating EIF2AK2 phosphorylation in macrophages. Antioxidant. Free radical scavenger. Directly inhibits nitric oxide synthase (NOS). Regulator of systemic glucose tolerance, energy balance and adiposity/obesity. Adipogenesis inhibitor. Shown to inhibit fat accumulation in adipocytes. Antibacterial and antifungal agent. Shown to potentially inhibit the 33.8-kDa Main Protease (Mpro)/3C-like Protease of SARS-CoV-2, consequently inhibiting viral transcription and replication and possibly inhibiting spread of COVID-19.

810.69 €

10-046

Tofacitinib

Potent cell permeable JAK3 inhibitor (IC50 = 1nM). Shows also JAK-1 inhibitory activity. Immunosuppressive and anti-inflammatory agent. Inhibits signaling through heterodimeric receptors associated with JAK3, JAK1, or both of them, with functional selectivity over JAK2-paired receptors. Blocks downstream STAT signaling, resulting in potent inhibition of several cytokines, including interleukins 2, 4, 7, 9, 15 and 21, which are integral to lymphocyte activation, function and proliferation. Investigated for several autoimmune disorders including, rheumatoid arthritis and psoriasis. Potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro. It is investigated against the spread of the SARS-CoV-2 (COVID-19). PRK1 inhibitor.

799.23 €

10-047