Vicriviroc Malate

Catalog No.S2004 Batch:S200402

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Technical Data

Formula

C28H38F3N5O2.C4H6O5
Molecular Weight 667.72 CAS No. 541503-81-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (149.76 mM)
Water 100 mg/mL (149.76 mM)
Ethanol 100 mg/mL (149.76 mM)
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)

References

  • https://pubmed.ncbi.nlm.nih.gov/16304152/

Customer Product Validation

<p>Effect of CCR5 receptor antagonists/ligands on LukED cytotoxicity and HIV infection. (a) Viability of Jurkat-R5 cells pre-incubated with CCR5 small molecule antagonists maraviroc (MVC), vicriviroc (VVC), or TAK-779 (TAK) (1μg/mL to 2.5 pg/mL) followed by incubation with LukED (5 μg/mL) and quantification of cell viability via FACS scatter. (b) HIV infection of Hut-R5 cells after incubation with the same CCR5 antago-nists as in (a) (1μg/mL to 64 pg/mL) and subsequent incubation with CCR5-tropic HIV-1 virus encoding the mouse heat-stable antigen (HSA) as a reporter (HIV-R5) for 2.5 days. Infection success was determined by FACS analysis after staining cells for the HSA protein encoded by the virus. Mean and s.e.m. of infected cells from duplicate experiments is shown.</p>

Data from [ Nature , 2013 , 493, 51-5 ]

<p>PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.</p><div><div> </div></div><p> </p>

Data from [ J Antimicrob Chemother , 2011 , 66, 802-812 ]

<p>mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.</p>

Data from [ J Antimicrob Chemother , 2011 , 66, 802-812 ]

<p>Effect of antiretrovirals and positive control rifampicin (at 10 μmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P<0.01.</p>

Data from [ J Antimicrob Chemother , 2011 , 66, 802-812 ]

Selleck's Vicriviroc Malate Has Been Cited by 4 Publications

CCR5 is a receptor for Staphylococcus aureus leukotoxin ED. [Alonzo F 3rd, et al. Nature, 2013, 493(7430):51-5] PubMed: 23235831
CCR5 antagonist blocks metastasis of basal breast cancer cells. [Velasco-Velázquez M, et al. Cancer Res, 2012, 72(15):3839-50] PubMed: 22637726
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro. [Zembruski NC, et al. J Antimicrob Chemot, 2011, 66(4):802-12] PubMed: 21393174
Decreased HIV diversity after allogeneic stem cell transplantation of an HIV-1 infected patient: a case report. [Kamp C, et al. Virol J, 2010, 7:55] PubMed: 20210988

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.