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Products
Pharmacology
Type
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- Technical support
- Resources
Maraviroc
Cat. No. CK-060
Structure:
4,4-Difluoro-N-[(1S)-3-[(1R,5S)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide
Other Names:
UK-427,857
Activity:
CCR5 antagonist
Maraviroc is a potent and selective CCR5 antagonist with potent anti-HIV activity. Maraviroc prevents HIV-1 gp120 binding to CCR5 with an IC50 of 6.4nM, preventing cell-cell fusion and HIV-1 entry. Maraviroc also inhibits CCL3 (MIP-1α) binding to CCR5, and possesses antinociceptive effects in a rat model of neuropathic pain. Maraviroc is a clinically useful antiretroviral drug, being shown to be effective at inhibiting HIV-1 entry into cells in humans, and is well tolerated. Additionally, as cancer cells express CCR5 receptors, maraviroc is able to block metastasis of basal breast and pancreatic cancer cells, induce cytotoxic and apoptotic effects in colorectal cancer cells, and reduce metastatic tumour growth in lungs. Maraviroc is also effective in models of graft-versus-host disease and inflammatory diseases.
Dorr et al (2005) Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother. 49(11) 4721 PMID: 16251317
Velasco-Velázquez et al (2012) CCR5 antagonist blocks metastasis of basal breast cancer cells. Cancer Res. 72(15) 3839 PMID: 22637726
Woollard and Kanmogne (2015) Maraviroc: a review of its use in HIV infection and beyond. Drug Des Devel Ther. 9 5447 PMID: 26491256
Zi et al (2017) Treatment with the C-C chemokine receptor type 5 (CCR5)-inhibitor maraviroc suppresses growth and induces apoptosis of acute lymphoblastic leukemia cells. Am J Cancer Res. 7(4) 869 PMID: 28469959
Aldinucci et al (2020) The CCL5/CCR5 Axis in Cancer Progression. Cancers (Basel) 12(7) 1765 PMID: 32630699
Related areas
All small molecules >
All chemokine receptor modulators >
All antivirals >
All cancer research categories >
All immunology research categories >
Technical Data
| Structure | 4,4-Difluoro-N-[(1S)-3-[(1R,5S)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide |
| CAS Number | 376348-65-1 |
| Molecular Weight | 513.68 |
| Formula | C29H41F2N5O |
Solubility and Storage
| Solubility | Soluble in DMSO to 25 mg/ml |
| Appearance | White solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >98% by HPLC, NMR conforms |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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