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Aplaviroc hydrochloride

Catalog No. T26642   CAS 461023-63-2
Synonyms: AK602, AK 602, GW873140A, GW-873140, GW873140, AK-602, Aplaviroc HCl

Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc selectively inhibits the binding of a particular monoclonal antibody, 45531, to CCR5.

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Aplaviroc hydrochloride Chemical Structure
Aplaviroc hydrochloride, CAS 461023-63-2
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 1,140.00
50 mg 10-14 weeks $ 1,490.00
100 mg 10-14 weeks $ 2,360.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc selectively inhibits the binding of a particular monoclonal antibody, 45531, to CCR5.
Targets&IC50 HIV-1 (MOKW):0.2 nM (IC50), HIV-1 (JRFL):0.1 nM (IC50), HIV-1 (Ba-L):0.4 nM (IC50)
Synonyms AK602, AK 602, GW873140A, GW-873140, GW873140, AK-602, Aplaviroc HCl
Molecular Weight 614.17
Formula C33H44ClN3O6
CAS No. 461023-63-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Latinovic O, Heredia A, Gallo RC, Reitz M, Le N, Redfield RR. Rapamycin enhances aplaviroc anti-HIV activity: implications for the clinical development of novel CCR5 antagonists. Antiviral Res. 2009 Jul;83(1):86-9. doi: 10.1016/j.antiviral.2009.02.199. Epub 2009 Mar 9. PubMed PMID: 19501260. 2. Yeni P, Lamarca A, Berger D, Cimoch P, Lazzarin A, Salvato P, Smaill FM, Teofilo E, Madison SJ, Nichols WG, Adkison KK, Bonny T, Millard J, McCarty D; EPIC (CCR100136) study team. Antiviral activity and safety of aplaviroc, a CCR5 antagonist, in combination with lopinavir/ritonavir in HIV-infected, therapy-naïve patients: results of the EPIC study (CCR100136). HIV Med. 2009 Feb;10(2):116-24. doi: 10.1111/j.1468-1293.2008.00660.x. PubMed PMID: 19200175. 3. Nolan KM, Del Prete GQ, Jordan AP, Haggarty B, Romano J, Leslie GJ, Hoxie JA. Characterization of a human immunodeficiency virus type 1 V3 deletion mutation that confers resistance to CCR5 inhibitors and the ability to use aplaviroc-bound receptor. J Virol. 2009 Apr;83(8):3798-809. doi: 10.1128/JVI.01751-08. Epub 2009 Feb 4. PubMed PMID: 19193800; PubMed Central PMCID: PMC2663279. 4. Kitrinos KM, Amrine-Madsen H, Irlbeck DM, Word JM, Demarest JF; CCR100136 Study Team. Virologic failure in therapy-naive subjects on aplaviroc plus lopinavir-ritonavir: detection of aplaviroc resistance requires clonal analysis of envelope. Antimicrob Agents Chemother. 2009 Mar;53(3):1124-31. doi: 10.1128/AAC.01057-08. Epub 2008 Dec 15. PubMed PMID: 19075068; PubMed Central PMCID: PMC2650553.

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Keywords

Aplaviroc hydrochloride 461023-63-2 AK602 Aplaviroc Hydrochloride AK 602 GW873140A GW-873140 GW873140 GW 873140 AK-602 Aplaviroc HCl inhibitor inhibit

 

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