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Aplaviroc hydrochloride Sale

(Synonyms: AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride) 目录号 : GC62610

Aplaviroc (AK 602) hydrochloride,SDP的一个衍生物,是 CCR5 的拮抗剂,其对 HIV-1Ba-L, HIV-1JRFL 和 HIV-1MOKW 的 IC50 值为 0.1-0.4 nM。

Aplaviroc hydrochloride Chemical Structure

Cas No.:461023-63-2

规格 价格 库存 购买数量
1 mg
¥5,220.00
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5 mg
¥8,550.00
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10 mg
¥14,850.00
现货
25 mg
¥31,050.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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

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. Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. 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). Aplaviroc 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. Aplaviroc potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM. 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].

The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly[2].Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice[2].

[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.
[2]. Hirotomo Nakata, et al. Potent anti-R5 human immunodeficiency virus type 1 effects of a CCR5 antagonist, AK602/ONO4128/GW873140, in a novel human peripheral blood mononuclear cell nonobese diabetic-SCID, interleukin-2 receptor gamma-chain-knocked-out AIDS mouse model. Virol. 2005 Feb;79(4):2087-96.

Chemical Properties

Cas No. 461023-63-2 SDF
别名 AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride
分子式 C33H44ClN3O6 分子量 614.17
溶解度 DMSO : 500 mg/mL (814.11 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.6282 mL 8.1411 mL 16.2821 mL
5 mM 0.3256 mL 1.6282 mL 3.2564 mL
10 mM 0.1628 mL 0.8141 mL 1.6282 mL
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Research Update

Discontinued drugs in 2005: anti-infectives

Expert Opin Investig Drugs 2007 Jan;16(1):1-10.PMID:17155849DOI:10.1517/13543784.16.1.1.

This perspective is the fifth in a series discussing drugs dropped from development in 2005, of which 11 were being developed for infectious diseases. Of these, eight were antivirals and were dropped in Phase II or III: Medivir's alovudine, Ono Pharmaceuticals' Aplaviroc hydrochloride and Excite's immunotherapeutic Xcellerate for HIV; Boehringer Ingelheim's ciluprevir, ViroPharma's HCV-086, Isis Pharmaceuticals' antisense oligonucleotide ISIS-14803, Japan Tobacco's JTK-003 and Rigel's R803 for hepatitis C virus. The remaining discontinued anti-infective drugs were an antibacterial vaccine (Vical's anthrax vaccine), an antiseptic (YM Bioscience's Dermofural) and an antifungal formulation (MacroChem's topical econazole). The drugs are grouped by compound class and reasons for their failure are discussed in this article.