A CCR5 antagonist (Ki = 2.5 nM); selectively inhibits CCR5 over M1 and M2 muscarinic acetylcholine receptors (Kis = >10

Vicriviroc (maleate) – 5 mg

Brand:
Cayman
CAS:
599179-03-0
Storage:
-20
UN-No:
Non-Hazardous - /

Vicriviroc is a chemokine (C-C motif) receptor 5 (CCR5) antagonist (Ki = 2.5 nM).{53315} It selectively inhibits CCR5 over M1 and M2 muscarinic acetylcholine receptors (Kis = >10,000 nM for both) and human-ether-a-go-go (hERG) potassium channels (IC50 = 5.8 µM).{53315} Vicriviroc decreases chemotaxis induced by chemokine (C-C motif) ligand 3 (CCL3) in Ba/F3 cells expressing recombinant human CCR5 with an IC50 value of 0.91 nM.{53316} It inhibits the replication of 30 R5-tropic HIV-1 clinical isolates in peripheral blood mononuclear cells (PBMCs; 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).  

 

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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

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