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Selonsertib {[allProObj[0].p_purity_real_show]}

货号:A156190 同义名: GS-4997;GS-4977

Selonsertib (GS-4997) 是一种口服可用和选择性的凋亡信号调节激酶 1 (ASK1) 抑制剂,pIC50 为 8.3,已被研究作为治疗糖尿病肾病和肾纤维化的潜在药物。

Selonsertib 化学结构 CAS号:1448428-04-3
Selonsertib 化学结构
CAS号:1448428-04-3
Selonsertib 3D分子结构
CAS号:1448428-04-3
Selonsertib 化学结构 CAS号:1448428-04-3
Selonsertib 3D分子结构 CAS号:1448428-04-3
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Selonsertib 纯度/质量文件 产品仅供科研

货号:A156190 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 MEK MEK1 MEK1/2 MEK2 MEK5 其他靶点 纯度
Honokiol 98%
Mirdametinib ++++

MEK, IC50: 0.33 nM

99%+
Binimetinib +++

MEK, IC50: 12 nM

99%+
BI-847325 ++

MEK1, IC50: 25 nM

+++

MEK2, IC50: 4 nM

99%+
U0126-EtOH +

MEK1, IC50: 0.07 μM

++

MEK2, IC50: 0.06 μM

98%
GDC-0623 ++++

MEK1, IC50: 0.13 nM

99%+
TAK-733 ++++

MEK1, IC50: 3.2 nM

99%+
Trametinib ++++

MEK1, IC50: 0.92 nM

++++

MEK2, IC50: 1.8 nM

99%+
Selumetinib +++

MEK1, Kd: 99 nM

MEK1, IC50: 14 nM

+

MEK2, Kd: 530 nM

99%+
CI-1040 ++

MEK1, IC50: 17 nM

++

MEK2, IC50: 17 nM

99%+
Myricetin 98%
Refametinib ++

MEK1, IC50: 19 nM

++

MEK2, IC50: 47 nM

99%+
Cobimetinib +++

MEK1, IC50: 4.2 nM

99%+
PD98059 +

MEK1, IC50: 2 μM

99%+
SL327 +

MEK1, IC50: 0.18 μM

+

MEK2, IC50: 0.22 μM

AP-1 98+%
PD318088 98%
AZD8330 +++

MEK1/2, IC50: 7 nM

99%+
Pimasertib 98%
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

99%+
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Selonsertib 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].
体外研究

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.

Selonsertib 动物研究

Dose Mice: 30 mg/kg[3] (p.o.), 15 mg/kg[4] (p.o.)
Administration p.o.

Selonsertib 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.

Selonsertib 实验方案

计算器
存储液制备 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

Selonsertib 技术信息

CAS号1448428-04-3
分子式C24H24FN7O
分子量 445.492
别名 GS-4997;GS-4977
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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