Formulation: A solid
Formal Name: 4,4-difluoro-N-[(1S)-3-[(3-exo)-3-[3-methyl-5-(1-(methyl-d3)ethyl-2,2,2-d3)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]-cyclohexanecarboxamide
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C29H35D6F2N5O
Formula Weight: 519,7
Shelf life (days): 1460
CAS Number: 1033699-22-7
Notes: Maraviroc-d6 is intended for use as an internal standard for the quantification of maraviroc (Item No. 14641). 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 chemokine (C-C motif) ligand 3 (CCL3), CCL4, and CCL5 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 for all), 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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