An orally bioavailable antagonist of CCR5 and CCR2 (IC50s = 2.3 and 5.9 nM

Cenicriviroc – 500 µg

Brand:
Cayman
CAS:
497223-25-3
Storage:
-20
UN-No:
Non-Hazardous - /

Cenicriviroc is an orally bioavailable antagonist of C-C chemokine receptor type 5 (CCR5) and CCR2 that inhibits binding of macrophage inflammatory protein 1α (MIP-1α; IC50 = 2.3 nM) and monocyte chemotactic protein 1 (MCP-1; IC50 = 5.9 nM), respectively, in CHO cells.{41586} Cenicriviroc is also an antagonist of CCR3 and CCR4 (IC50s = 2.4 and 1.1 μM, respectively), however, it does not inhibit agonist binding to CCR1 or CCR7 at concentrations up to 10 μM. At a concentration of 100 nM, cenicriviroc completely inhibits replication of R5 HIV-1 in U87.CD4.CCR5 cells. Cenicriviroc inhibits replication of the R5 HIV-1 strains JR-FL and KK in peripheral blood mononuclear cells (PBMCs) with EC50 values ranging from 21 to 210 pM and 33 to 91 pM, respectively. In vivo, cenicriviroc (20 mg/kg per day) reduces collagen deposition, levels of collagen type 1 protein and mRNA expression, and non-alcoholic fatty liver disease activity score in a mouse model of non-alcoholic steatohepatitis (NASH).{41587} It also reduces collagen type 1 protein levels, mRNA expression, and collagen deposition in a mouse model of unilateral ureter obstruction and a rat model of thioacetamide-induced liver fibrosis.  

 

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SKU: 23927 - 500 µg Category:

Description

An orally bioavailable antagonist of CCR5 and CCR2 (IC50s = 2.3 and 5.9 nM, respectively, for receptors in CHO cells); an antagonist of CCR3 and CCR4 (IC50s = 2.4 and 1.1 μM, respectively); completely inhibits replication of R5 HIV-1 in U87.CD4.CCR5 cells (100 nM); inhibits replication of the R5 HIV-1 strains JR-FL and KK in PBMCs (EC50s = 21-210 pM and 33-91 pM, respectively); reduces collagen deposition, levels of collagen type 1 protein and mRNA expression, and non-alcoholic fatty liver disease activity score in a mouse model of NASH (20 mg/kg per day); reduces collagen type 1 protein levels, mRNA expression, and collagen deposition in a mouse model of unilateral ureter obstruction and a rat model of thioacetamide-induced liver fibrosis

Formal name: 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4-[(S)-[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-1-benzazocine-5-carboxamide

Synonyms:  TAK-652

Molecular weight: 696.9

CAS: 497223-25-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|CCR5 Receptor Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease|Viral Diseases|HIV & AIDS

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