Maraviroc

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 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
• Correlated keywords
  • 674782-29-7 receptors antagonists antivirals HIV infections infectious diseases anti virals anti-viral C-C chemokines types 5 binding binds binder ligands RANTES regulated activations normal Ts cells T-cells Tcells expressed secreted humans immunodeficiency virus HIV-1 UKs 427857 UK-427857 UK427857 celsentri selzentry maraviroc CCR5 inhibiting inhibitors inhibitions inhibits monocytes macrophages replications expressing pharmacokinetics healthy males delineated Celsentri Selzentry
• Product Overview:
  Maraviroc is an antagonist of chemokine (C-C motif) receptor 5 (CCR5; Ki = 0.24 nM for the rhesus monkey recombinant receptor).{45486} It inhibits binding of MIP-1?, MIP-1?, 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}