产品说明书

Selonsertib

Print
Chemical Structure| 1448428-04-3 同义名 : GS-4997;GS-4977
CAS号 : 1448428-04-3
货号 : A156190
分子式 : C24H24FN7O
纯度 : 99%+
分子量 : 445.492
MDL号 : MFCD29920355
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(67.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

生物活性
靶点

  • ASK1

    ASK1, pIC50:8.3
描述 Selonsertib (GS-4997) is identified as an ASK1 inhibitor under clinical evaluation, proposed as a novel therapeutic for diabetic nephropathy and kidney fibrosis[1]. Selonsertib (GS-4997) is characterized as a highly selective and potent ASK1 inhibitor that operates through competitive inhibition with ATP within the catalytic kinase domain of ASK1, offering potential therapeutic benefits when administered once daily orally[2].
作用机制 GS-4997 binds to the catalytic domain of ASK1 in an ATP-competitive manner thus preventing phosphorylation and activation.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.22mL

2.24mL

1.12mL

22.45mL

4.49mL

2.24mL
参考文献

[1]Lanier M, et al. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure. ACS Med Chem Lett. 2017 Feb 8;8(3):316-320.

[2]Lin JH, et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129(1):29-33.