A CCR5 antagonist (Ki = 0.24 nM for the rhesus monkey recombinant receptor); inhibits binding of MIP-1α

Maraviroc – 50 mg

Brand:
Cayman
CAS:
376348-65-1
Storage:
-20
UN-No:
Non-Hazardous - /

Maraviroc is an antagonist of the chemokine (C-C motif) receptor 5 (CCR5; Ki = 0.24 nM for the rhesus monkey recombinant receptor).{45486} It inhibits binding of MIP-1α, MIP-1β, and RANTES to HEK293 cell membranes expressing CCR5 (IC50s = 3.3, 7.2, and 5.2 nM, respectively) and inhibits HIV-1 binding to CCR5 via glycoprotein 120 (gp120) and gp160 (IC50s = 11 and 0.22 nM, respectively).{45484} Maraviroc is selective for CCR5 over CCR1, -2, -3, -4, -7, and -8, and chemokine (C-X-C motif) receptor 1 (CXCR1) and CXCR2 in a panel of immunological assays for ligand-induced cell chemotaxis and ligand-receptor binding (IC50s = >10 µM for all). It has antiviral activity against laboratory and clinical isolates of CCR5-tropic (IC50s = 0.1-1.1 nM), but not CXCR4-tropic or dual tropic (IC50s = >10 µM), HIV-1 in isolated human peripheral blood mononuclear cells (PBMCs). Maraviroc prevents infection upon exposure to HIV-1 in humanized RAG-hum mice when administered at a dose of 62 mg/kg.{45485}  

 

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Description

A CCR5 antagonist (Ki = 0.24 nM for the rhesus monkey recombinant receptor); inhibits binding of MIP-1α, MIP-1β, and RANTES to HEK293 cell membranes expressing CCR5 (IC50s = 3.3, 7.2, and 5.2 nM, respectively) and inhibits HIV-1 binding to CCR5 via gp120 and gp160 (IC50s = 11 and 0.22 nM, respectively); selective for CCR5 over CCR1, -2, -3, -4, -7, and -8, and CXCR1 and CXCR2 in a panel of immunological assays for ligand-induced cell chemotaxis and ligand-receptor binding (IC50s = >10 µM for all); has antiviral activity against laboratory and clinical isolates of CCR5-tropic (IC50s = 0.1-1.1 nM), but not CXCR4-tropic or dual tropic (IC50s = >10 µM), HIV-1 in isolated human PBMCs; prevents infection upon exposure to HIV-1 in humanized RAG-hum mice at 62 mg/kg

Formal name: 4,4-difluoro-N-[(1S)-3-[(3-exo)-3-[3-methyl-5-(1-methylethyl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]-cyclohexanecarboxamide

Synonyms:  UK 427857

Molecular weight: 513.7

CAS: 376348-65-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|CCR5 Receptor Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease|Viral Diseases|HIV & AIDS

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