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Maraviroc is an antiretroviral compound in the CCR5 receptor antagonist class used in the treatment of HIV infection. It is also classed as an entry inhibitor. Maraviroc is extensively metabolized by CYP3A4, with renal clearance accounting for approximately 23% of total clearance. Maraviroc is an entry inhibitor. Specifically, maraviroc is a negative allosteric modulator of the CCR5 receptor, which is found on the surface of certain human cells. Maraviroc (UK-427857) inhibits CCL3 (MIP-1α) binding to CCR5, thereby blocking the HIV protein gp120 from associating with the receptor. Maraviroc (brand-named Selzentry, or Celsentri) displays potent anti-HIV-1 activity. UK-427857 prevents the interaction of HIV-1 gp120 and CCR5 (IC50 = 6.4 nM), inhibiting HIV-1 entry. Maraviroc has no detectable in vitro cytotoxicity and is highly selective for CCR5, as confirmed against a wide range of receptors and enzymes, including the hERG ion channel (50% inhibitory concentration, >10 μM), indicating potential for an excellent clinical safety profile. Maraviroc also appeared to reduce graft-versus-host disease in patients treated with allogeneic bone marrow transplantation for leukemia, in a phase 1/2 study. In addition, those who received the entry inhibitor had a mean increase in CD4 cells of 110 cells/µL in the once-daily group, 106 cells/µL in the twice-daily group, and 56 cells/µL in the placebo group.
Acta Neuropathol Commun. 2024 Sep 10;12(1):147.
Protein phosphatase 2Cm-regulated branched-chain amino acid catabolic defect in dorsal root ganglion neurons drives pain sensitization
Maraviroc purchased from AbMole
Acta Neuropathol Commun. 2024 Sep 10;12(1):147.
Protein phosphatase 2Cm-regulated branched-chain amino acid catabolic defect in dorsal root ganglion neurons drives pain sensitization
Maraviroc purchased from AbMole
Patent. CN113512587A 2021 Oct 19.
Patent. CN113512587A
Maraviroc purchased from AbMole
| Molecular Weight | 513.67 |
| Formula | C29H41F2N5O |
| CAS Number | 376348-65-1 |
| Solubility (25°C) | DMSO 50 mg/mL Ethanol 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CCR Products |
|---|
| Vicriviroc Malate
Vicriviroc (SCH 417690) is a pyrimidine CCR5 entry inhibitor of HIV-1 with IC50 of 0.91 nM. |
| Bindarit
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Bindarit also has anti-inflammatory activity. |
| BMS-813160
BMS-813160 is the first dual CCR2/CCR5 antagonist. BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively. |
| INCB3284 dimesylate
INCB 3284 dimesylate is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM. |
| BX 471
BX 471 is a potent, selective CCR1 antagonist. |
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