Aplaviroc hydrochloride (GSK-873140) | CCR5 inhibitor

Chemical Structure : Aplaviroc hydrochloride

Aplaviroc hydrochloride (AK-602, GW 873140, ONO-4128, GSK-873140)

Catalog No.: PC-62992Not For Human Use, Lab Use Only.

Aplaviroc hydrochloride (GSK-873140;GW 873140;AK-602;ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6.

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Biological Activity

Aplaviroc hydrochloride (GSK-873140;GW 873140;AK-602;ONO-4128) is a potent, noncompetitive, allosteric antagonist of the CCR5 receptor with pKb of 8.6.
Aplaviroc blocks the calcium response effects of CCR5 activation by CCL5, and potently blocks in vitro the infection of R5-tropic HIV-1 (R5-HIV-1) at subnanomolar IC50.

Physicochemical Properties

M.Wt	614.18
Formula	C33H44ClN3O6
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-[4-[[(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undecan-9-yl]methyl]phenoxy]benzoic acid hydrochloride

References

1. Watson C, et al. Mol Pharmacol. 2005 Apr;67(4):1268-82.

2. Lalezari J, et al. AIDS. 2005 Sep 23;19(14):1443-8.

3. Adkison KK, et al. Antimicrob Agents Chemother. 2005 Jul;49(7):2802-6.

4. Nakata H, et al. Antimicrob Agents Chemother. 2008 Jun;52(6):2111-9.

Aplaviroc hydrochloride (AK-602, GW 873140, ONO-4128, GSK-873140)

Biological Activity

Physicochemical Properties

References

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