Maraviroc, CCR5 antagonist (TBI4260)

Description

Product Details

Formal Name: 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

Alternate Names: UK-427,857

Molecular Formula: C₂₉H₄₁F₂N₅O

Formula Weight: 513.70

CAS Number: 376348-65-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

CCR5 antagonist

Functions

Potent and selective CCR5 antagonist with strong anti-HIV activity. Prevents HIV-1 gp120 binding to CCR5, preventing cell-cell fusion. Inhibited MIP-1a (IC50 = 3.3 nM), MIP-1b (IC50 = 7.2 nM), and RANTES (IC50 = 5.2 nM) binding to CCR5-expressing HEK-293 cells. Clinically useful antiretroviral drug. Many cancer cells express CCR5: Maraviroc blocks metastasis of basal breast and pancreatic cancer cells, induces cytotoxic and apoptotic effects in colorectal cancer cells, reduces metastatic tumor growth in lungs, and suppresses growth in acute ALL cells. CCR inhibition with maraviroc induces macrophage repolarization with anti-tumoral effects.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.