Maraviroc

  • Chemical Properties
CAS No. 376348-65-1 Cat. No. BCP01819
Name Maraviroc
Synonyms UK-427857;Celsentri;UK427857;UK 427857;
Formula C29H41F2N5O M. Wt 513.67
  • Biological Activity
Description Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CCR5/G protein complex. Maraviroc also inhibits the downstream event of chemokine-induced intracellular calcium redistribution, with IC50s ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES. In the same experiments, Maraviroc does not trigger release of intracellular calcium at concentrations up to 10 μM, indicating that it is devoid of CCR5 agonist activity. Consistent with this, Maraviroc fails to induce CCR5 internalization. Maraviroc is active at low nanomolar concentrations against HIV-1 Ba-L. Maraviroc inhibits all 200 pseudotyped viruses with a geometric mean IC90 of 13.7 nM.
Pathways Microbiology/Virology GPCR/G Protein 
Targets HIV CCR 

Structure

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