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Aplaviroc

Chemical Structure Aplaviroc

CAS No.: 461443-59-4

Aplaviroc (AK-602;GW 873140;ONO-4128;GSK-873140)

Catalog No.: PC-61968Not For Human Use, Lab Use Only.

Aplaviroc (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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

HIV Infection

Phase 3 Discontinued

Physicochemical Properties

M.Wt 577.722
Formula C33H43N3O6
CAS No. 461443-59-4
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name

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

Clinical Information

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.

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