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Vicriviroc is an orally available CCR5 antagonist, which binds specifically to the CCR5 receptor and prevents infection of target cells by CCR5-tropic HIV-1 isolates. Vicriviroc potently inhibited all the viral isolates tested, with geometric mean EC50s ranging between 0.04 nM and 2.3 nM and IC90s between 0.45 nM and 18 nM. Vicriviroc inhibits MIP-1α induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. Vicriviroc inhibits GTPγS binding to the membranes from HTS-hCCR5 cells induced by RANTES, with IC50 of 4.2 nM. Competition binding assays revealed that vicriviroc binds with higher affinity to CCR5 than SCH-C. Finally, vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects.
| Molecular Weight | 667.72 |
| Formula | C28H38F3N5O2.C4H6O5 |
| CAS Number | 541503-81-5 |
| Solubility (25°C) | Water |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CCR Products |
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| Maraviroc
Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. |
| Bindarit
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Bindarit also has anti-inflammatory activity. |
| BMS-813160
BMS-813160 is the first dual CCR2/CCR5 antagonist. BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively. |
| INCB3284 dimesylate
INCB 3284 dimesylate is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM. |
| BX 471
BX 471 is a potent, selective CCR1 antagonist. |
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