GSK3395879

• 常用名: GSK3395879
• 英文名: GSK3395879
• CAS号: 2215852-91-6
• 分子量: 485.41
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₅F₄N₃O₅S
• 熔点: N/A
• 闪点: N/A

GSK3395879用途

GSK3395879 是一种口服生物可利用的选择性瞬时受体电位香草醛-4 (TRPV4) 拮抗剂,作用于 hTRPV4,IC50 为 1 nM。

GSK3395879名称

• 中文名: GSK3395879
• 英文名: GSK3395879

GSK3395879生物活性

• 描述: GSK3395879 是一种口服生物可利用的选择性瞬时受体电位香草醛-4 (TRPV4) 拮抗剂,作用于 hTRPV4,IC50 为 1 nM。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 心血管疾病
• 靶点实验:

  IC50: 1 nM (hTRPV4)[1]

• 参考文献:

  [1]. Brnardic EJ, et al. Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem. 2018 Nov 8;61(21):9738-9755.

GSK3395879物理化学性质

• 分子式: C₂₀H₁₅F₄N₃O₅S
• 分子量: 485.41
• InChIKey: RAYCYIKGBWRQBC-RBUKOAKNSA-N
• SMILES: N#Cc1ccc(OC2CN(S(=O)(=O)c3ccc(C(F)(F)F)cc3C#N)CC2(O)CO)cc1F

GSK3395879靶点实验

查看更多实验

实验名称：Ratio of Cmax to Cmin in human 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322961

实验名称：Drug metabolism in rat hepatocytes assessed as oxidation of arene oxide metabolite by... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322958

实验名称：Drug metabolism in rat hepatocytes assessed as rearomatization/conjugation by measuri... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322957

实验名称：Drug metabolism in rat hepatocytes assessed as GSH-mediated sulfonamide cleavage by m... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322956

实验名称：Ratio of unbound clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as 30 mi... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322955

实验名称：In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4158460

实验名称：In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4158461

实验名称：In vivo antagonist activity at TRPV4 in iv dosed Sprague-Dawley rat assessed as inhib... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4158462

实验名称：Oral bioavailability in Sprague-Dawley rat at 1 mg/kg by HPLC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322943

实验名称：Dose normalized AUC in Sprague-Dawley rat at 1 mg/kg, po by HPLC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL4322942

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