Description
A CCR5 antagonist (Ki = 2.5 nM); selectively inhibits CCR5 over M1 and M2 muscarinic acetylcholine receptors (Kis = >10,000 nM for both) and hERG potassium channels (IC50 = 5.8 µM); decreases CCL3-induced chemotaxis of Ba/F3 cells expressing recombinant human CCR5 (IC50 = 0.91 nM); inhibits the replication of 30 R5-tropic HIV-1 clinical isolates in PMBCs (EC50s = 0.04-1.4 nM) and reduces viral entry of seven drug-resistant strains of HIV-1 in U87 cells expressing CD4 and CCR5 (EC50s = 8.7-32.9 nM)
Formal name: 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methyl-1-piperazinyl]-4-methyl-piperidine, 2Z-butenedioate
Synonyms: SCH 417690
Molecular weight: 649.7
CAS: 599179-03-0
Purity: ≥98%
Formulation: A crystalline solid
