
Aplaviroc
CAS No. 461443-59-4
Aplaviroc ( AK-602 | GW 873140 | ONO-4128 | GSK-873140 )
产品货号. M14555 CAS No. 461443-59-4
Aplaviroc (GSK-873140;GW 873140;AK-602;ONO-4128) 是一种有效的、非竞争性的 CCR5 受体变构拮抗剂。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥12717 | 有现货 |
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50MG | ¥25758 | 有现货 |
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100MG | ¥34830 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称Aplaviroc
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述Aplaviroc (GSK-873140;GW 873140;AK-602;ONO-4128) 是一种有效的、非竞争性的 CCR5 受体变构拮抗剂。
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产品描述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.
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体外实验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.
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体内实验The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly.Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice. Animal Model:hu-PBMC-NOG mice.Dosage:60 mg/kg.Administration:Single intraperitoneal administration, bid, daily.Result:The numbers of CD4+ cells/μL in saline-treated mice were significantly less than those of AK602-treated, ddI-treated, or uninfected mice.
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同义词AK-602 | GW 873140 | ONO-4128 | GSK-873140
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通路GPCR/G Protein
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靶点Chemokine Receptor
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受体Chemokine Receptor
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研究领域Infection
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适应症HIV Infection
化学信息
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CAS Number461443-59-4
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分子量577.722
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分子式C33H43N3O6
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纯度>98% (HPLC)
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溶解度——
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SMILESO=C(O)C1=CC=C(OC2=CC=C(CN(CC3)CCC3(N(CCCC)C([C@@H]([C@@H](C4CCCCC4)O)N5)=O)C5=O)C=C2)C=C1
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化学全称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
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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.
产品手册




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