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Aplaviroc

Catalog No. T14307 CAS 461443-59-4

Synonyms: AK 602, GW 873140, GSK 873140

Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.

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Aplaviroc, CAS 461443-59-4

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 2,420.00
50 mg	10-14 weeks	$ 3,180.00
100 mg	10-14 weeks	$ 4,300.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
Targets&IC50	CCR5:, HIV-1 (JRFL):0.1 nM, HIV-1 (Ba-L):0.4 nM, HIV-1 (MOKW):0.2 nM
In vitro	Aplaviroc (AK602) is identified as the most potent agent among newly designed and synthesized SDP derivatives and it also is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW) with IC50 values of 0.1 to 0.4 nM and it potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM. The activity of Aplaviroc's anti-HIV-1 is limited and similar to that seen for zidovudine. Aplaviroc suppresses the infectivity and replication of two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at extremely low concentrations (IC50 values of 0.4 to 0.6 nM), while these two R5 HIV-1 variants are less susceptible to zidovudine, nelfinavir, and saquinavir and it also binds to CCR5 with high affinity. The Kd values thus determined for Aplaviroc, E913, E921/TAK-779, and AK671/SCH-C are 2.9±1.0, 111.7±3.5, 32.2±9.6, and 16.0±1.5 nM, respectively. These results suggest that the potent activity of Aplaviroc against R5 HIV-1 stems from its binding to ECL2B and/or its vicinity with high affinity, resulting in inhibition of gp120/CD4 binding to CCR5[1].

Synonyms	AK 602, GW 873140, GSK 873140
Molecular Weight	577.71
Formula	C33H43N3O6
CAS No.	461443-59-4

Storage

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

References and Literature

1. Maeda K, et al. Spirodiketopiperazine-based CCR5 inhibitor which preserves CC-chemokine/CCR5 interactions and exerts potent activity against R5 human immunodeficiency virus type 1 in vitro. J Virol. 2004 Aug;78(16):8654-62.

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Keywords

Aplaviroc 461443-59-4 Immunology/Inflammation Microbiology/Virology Proteases/Proteasome HIV Protease CCR AK 602 GW 873140 AK-602 AK602 GW-873140 GSK 873140 GSK-873140 GSK873140 GW873140 inhibitor inhibit

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