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首页- Products - Membrane Transporter/Ion Channel - Sodium Channel - PF-05089771

PF-05089771

CAS No. 1430806-04-4

PF-05089771 ( PF05089771 )

产品货号. M11822 CAS No. 1430806-04-4

PF-05089771 是一种有效的、状态依赖性、亚型选择性 Nav1.7 抑制剂，IC50 为 11 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ￥1017 有现货
10MG ￥1454 有现货
25MG ￥3395 有现货
500MG 获取报价 有现货
1G 获取报价 有现货
产品询价 大包装询价 加入购物车

生物学信息

  • 产品名称
    PF-05089771
  • 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
    PF-05089771 是一种有效的、状态依赖性、亚型选择性 Nav1.7 抑制剂，IC50 为 11 nM。
  • 产品描述
    PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8; interacts with the voltage-sensor domain (VSD) of domain IV, blocks all Nav1.7 splice variants with similar potency (5N11L, 5A11S, 5A11L and 5N11S, IC50s=11=33 nM); displays high selectivity over L-type calcium channels, KvLQT and hERG potassium channels; demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.
  • 体外实验
    PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4).PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5) whilst 100 nM resulted in complete block.
  • 体内实验
    ——
  • 同义词
    PF05089771
  • 通路
    Membrane Transporter/Ion Channel
  • 靶点
    Sodium Channel
  • 受体
    Na(V1.7) channel
  • 研究领域
    Neurological Disease
  • 适应症
    Pain

化学信息

  • CAS Number
    1430806-04-4
  • 分子量
    500.344
  • 分子式
    C18H12Cl2FN5O3S2
  • 纯度
    >98% (HPLC)
  • 溶解度
    ——
  • SMILES
    CC1=CC=C(C=C1)S(=O)(=O)O.C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F
  • 化学全称
    4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide

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. Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042. 2. Theile JW, et al. Mol Pharmacol. 2016 Nov;90(5):540-548. 3. Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405. 4. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801.
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