• 咨询热线
    客服服务热线 13671568941/15317326293
  • 在线咨询
  • 微信客服
    微信客服
  • 公众号
    扫码关注公众号

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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥12717 有现货
50MG ¥25758 有现货
100MG ¥34830 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    Aplaviroc
  • 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
  • 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。
  • 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.
  • 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.
  • 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.
  • 同义词
    AK-602 | GW 873140 | ONO-4128 | GSK-873140
  • 通路
    GPCR/G Protein
  • 靶点
    Chemokine Receptor
  • 受体
    Chemokine Receptor
  • 研究领域
    Infection
  • 适应症
    HIV Infection

化学信息

  • CAS Number
    461443-59-4
  • 分子量
    577.722
  • 分子式
    C33H43N3O6
  • 纯度
    >98% (HPLC)
  • 溶解度
    ——
  • SMILES
    O=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
  • 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

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 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
关联产品
  • AZ 13381758

    一种有效的小分子 CXCR2 抑制剂,对 mCXCR2 和 hCXCR2 的 IC50 分别为 26 nM 和 30 nM。

  • KRH-1636

    一种有效的、选择性的 CXCR4 抑制剂,IC50 为 13 nM。

  • MK-0812 succinate

    一种有效的 CCR2 特异性拮抗剂,可阻断 MCP-1 介导的反应,IC50 为 3.2 nM。