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S81464

BMS-378806

源葉(MedMol) 98%
  • 英文名:
  • BMS-378806
  • 別名:
  • BMS-378806;BMS-806
  • CAS號:
  • 357263-13-9
  • 分子式:
  • C22H22N4O4
  • 分子量:
  • 406.43
  • 核磁/質譜:
品牌貨號產品規(guī)格價格(RMB) 庫存(上海) 北京 武漢 南京 數(shù)量計量單位 加入購物車...
源葉(MedMol) S81464-5mg 98% ¥765.00元 6 - - - EA 加入購物車
源葉(MedMol) S81464-10mg 98% ¥1020.00元 7 - - - EA 加入購物車
源葉(MedMol) S81464-25mg 98% ¥2040.00元 6 - - - EA 加入購物車
源葉(MedMol) S81464-100mg 98% ¥6120.00元 預計交期:2-3天 - - - EA 加入購物車
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  • 提示:詳情請下載說明書。
  • 產品描述:

    BMS-378806 是一種有效的 HIV-1 抑制劑,干擾 CD4-gp120 相互作用。BMS-378806選擇性抑制 HIV-1 gp120 結合到 CD4 受體,EC50 為 0.85-26.5 nM。

  • 靶點: HIV-1;HIV-2;gp120/CD4;?HIVProtease
  • 體外研究:
    In a series of biochemical assays, BMS-378806 is not an effective inhibitor of HIV integrase, protease, or reverse transcriptase, but did compete with soluble CD4 binding to a monomeric form of gp120 in an ELISA assay with IC50=100 nM. The specificity of BMS-378806 toward inhibition of HIV-1 is confirmed by evaluation against HIV-2, SIV, MuLV, RSV, HCMV, BVDV, VSV, and influenza virus, with no significant inhibitory activity observed at concentrations ranging from 10 to 30 μM and no overt cytotoxicity toward the host cells, CC50>225 μM. BMS-378806 is not a potent inhibitor of any of the five major human CYP isoforms, evaluated as recombinant preparations, with IC50 values of >100 μM for CYP1A2 and CYP2C9, 23 μM for CYP2C19, 20 μM for CYP2D6, and 39 to 81 μM for CYP3A4. Moreover, since BMS-378806 is metabolized by CYP450 1A2, 2D6, and 3A4, it is unlikely to lead to severe drug?drug interactions in a clinical setting. BMS-378806 inhibits viral replication by interfering with the binding interactions of gp120 with the cellular CD4 receptor. The IC50s determined for the gp120s from HIV LAI, BAL, NA420LN40, SF162, NL4-3, NA420B33, YU2, AD8, JRCSF, and 92US15.6 are 0.1, 0.1, 0.3, 0.5, 0.6, 0.7, 0.9, 1.0, 1.1, and 1.6 μM, respectively. A similar observation is also made for BMS-378806 (IC50s range from 0.2 to 9.6 μM). BMS-378806 binds directly to gp120 at a stoichiometry of approximately 1:1, with a binding affinity similar to that of soluble CD4. The potential BMS-378806 target site is localized to a spec
  • 體內研究:
    In toxicology studies, BMS-378806 is well tolerated in rats at doses of 100 mg/kg/day for 2 weeks and in dogs at doses of 90 mg/kg for 10 days. The dose-proportional increases in the AUC and Cmax are observed between doses of 5 and 25 mpk, when BMS-378806 is administered either in the solution or suspension formulation. In all three species, plasma levels of drug exceeded the concentrations required to half-maximally inhibit virus replication in vitro. The volume of distribution of BMS-378806 ranges from 0.4 to 0.6 L/kg, indicative of partitioning beyond plasma; however, examination of brain levels in the rat reveals minimal CNS penetration.
  • 參考文獻:
    1. Wang T, et al. Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J Med Chem. 2003 Sep 25;46(20):4236-9.

    2. Ho HT, et al. Envelope conformational changes induced by human immunodeficiency virus type 1 attachment inhibitors prevent CD4 binding and downstream entry events. J Virol. 2006 Apr;80(8):4017-25.

    3. Guo Q, et al. Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J Virol. 2003 Oct;77(19):10528-36
  • 溶解性: Soluble  in  DMSO
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 2.46 ml 12.302 ml 24.604 ml
    5 mM 0.492 ml 2.46 ml 4.921 ml
    10 mM 0.246 ml 1.23 ml 2.46 ml
    50 mM 0.049 ml 0.246 ml 0.492 ml
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