Vicriviroc Malate

CAS NO

541503-81-5

Formula

C28H38F3N5O2.C4H6O5

Solubility

DMSO

Storage

at -20℃ 2 years

Weight

667.72

Biological Activity

In order to determine if vicriviroc is a receptor agonist or antagonist, three functional assays were employed to measure the ability of the compound to block b-chemokine signaling in CCR5-expressing cells.A chemotaxis assay was first employed to determine the ability of vicriviroc to inhibit chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human CCR5. In this assay,vicriviroc showed equally potent inhibition of the chemotactic response to MIP-1 with IC50 values below 1 nM. The ability of vicriviroc to inhibit intracellular calcium release induced by receptor stimulation was also assessed. A assay utilized to demonstrate the ability of vicriviroc to inhibit CCR5 receptor signaling was a GTPS exchange assay. GTPS binding induced by RANTES. vicriviroc potently inhibited RANTES-induced signaling with mean IC50s of 4.2 nM. [1]

References

[1] Julie M. Strizki et al. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9