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Medchemexpress LLC Vicriviroc maleate | 599179-03-0 | MFCD09833218 | >99.91% | 649.70 | 50 MG

Supplier: Medchemexpress LLC HY1737750MG
Vicriviroc maleate is a potent, selective, oral bioavailable, and central nervous system (CNS) penetrated antagonist of CCR5, with a Ki of 2.5 nM. It also inhibits HIV-1 in peripheral blood mononuclear cells (PBMC).
- Potent and selective CCR5 antagonist.
- Oral bioavailable and CNS penetrated.
- Inhibits HIV-1 in PBMC cells.
- Shows mean IC50 of 0.45 nM and IC90 of 4 nM for a panel of HIV isolates.
- Exhibits weak activity against hERG (IC50, 5.8 μM).
- Inhibits chemotactic response to MIP-1α with IC50 values below 1 nM.
- Suppresses RANTES-induced signaling with a mean IC50 of 4.2 ± 1.3 nM.
- Potently suppresses tested viral isolates with geometric mean EC50s of 0.04-2.3 nM and IC90s of 0.45-18 nM.
- Demonstrates good oral availability in rats and monkeys, with no acute CNS or GI effects at 10 mg/kg dose.
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