Vicriviroc Malate

Catalog No.S2004 Synonyms: SCH 417690 (SCH-D) Malate

For research use only.

Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.

Vicriviroc Malate Chemical Structure

CAS No. 541503-81-5

Selleck's Vicriviroc Malate has been cited by 4 Publications

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Biological Activity

Description Vicriviroc is a potent CCR5 antagonist with IC50 of 0.91 nM, showing broad-spectrum activity against genetically diverse HIV-1 isolates, and also drug-resistant viruses with RTI, PRI, or MDR phenotypes. Phase 3.
In vitro

Vicriviroc binds with higher affinity to CCR5 versus SCH-C (SCH-351125) in competition binding assays with Ki value of 0.8 nM versus 2.6 nM. Vicriviroc is nearly 6-fold less active than SCH-C (IC50 = 5.8 μM versus 1.1 μM) in attenuating hERG current among voltage-clamped L929 cells, indicating a reduced potential for cardiac effects. Vicriviroc inhibits MIP-1α induced migration of Ba/F3 cells stably expressing recombinant human CCR5, with IC50 of 0.91 nM. In U-87-CCR5 cells, Vicriviroc inhibits intracellular calcium release induced by the ligand RANTES with IC50 of 16 nM, while Vicriviroc treatment alone does not stimulate the release of calcium. Vicriviroc inhibits GTPγS binding to the membranes from HTS-hCCR5 cells induced by RANTES, with IC50 of 4.2 nM. Vicriviroc displays potent antiviral activity against a panel of 30 R5-tropic HIV-1 isolates representing diverse genetic clades, with EC50 values ranging from 0.04 nM to 2.3 nM, and EC90 from 0.45 nM to 18 nM, being more potent (2- to 40-fold) than SCH-C. Vicriviroc is also highly active against a Clade G Russian isolate RU570 with EC90 of 16 nM, which is resistant to inhibition by SCH-C (EC90 > 1 μM). Vicriviroc could target an early step in the viral life cycle prior to reverse transcription and virion maturation, the targets of reverse transcriptase inhibitor and protease inhibitor, respectively. Consistent with the selectivity for CCR5, Vicriviroc is not active against viruses capable of using the CXCR4 coreceptor (R5/X4 or X4 tropic) for infection. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 134 mg/mL
(200.68 mM)
Water 38 mg/mL
(56.91 mM)
Ethanol '134 mg/mL

Chemical Information

Molecular Weight 667.72
Formula

C28H38F3N5O2.C4H6O5

CAS No. 541503-81-5
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03631407 Completed Drug: Vicriviroc|Biological: Pembrolizumab Colorectal Neoplasms Merck Sharp & Dohme Corp. September 24 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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