Selonsertib (GS-4997)
(Synonyms: GS-4997) 目录号 : GC12124
An ASK1 inhibitor
Cas No.:1448428-04-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Selonsertib (GS-4997) is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor.
ASK1, a redox-sensitive mitogen-activated protein kinase kinase kinase, functions as a key signaling node by promoting deleterious effects. ASK1 activation can cause downstream activation of the terminal MAPK kinases p38 and c-Jun N-terminal kinase, which stimulate production of inflammatory cytokines, induce fibrosis, promote apoptotic and necrotic cell death, increase aberrant cell proliferation, as well as contribute to metabolic perturbations.
In vitro: GS-4997 has been identified as a highly selective and potent ASK1 inhibitor that competed with ATP in the ASK1 catalytic kinase domain. Moreover, the ASK1 inhibition caused by GS-4997 was found to be significantly different in mechanism from bardoxolone methyl. GS- 4997 could also shut down cell signaling involved in pathogenesis, while bardoxolone methyl activated mRNA transcription in every cell exposed to drug. In addition, GS-4997 could selectively target affected cells in which the oxidative burden was high [1].
In vivo: So far, there is no animal in vivo data released.
Clinical trial: The phase II study regarding delineating study population, efficacy outcomes, treatment period as well as statistical methods to resolve specific challenges for DKD study has been designed based on the biology of oxidative stress signaling through ASK1, the biology of DKD pathogenesis, and solid statistical methods [1].
Reference:
[1] 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.
| Cas No. | 1448428-04-3 | SDF | |
| 别名 | GS-4997 | ||
| 化学名 | 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide | ||
| Canonical SMILES | O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F | ||
| 分子式 | C24H24FN7O | 分子量 | 445.49 |
| 溶解度 | ≥ 44.5 mg/mL in DMSO, ≥ 88.8 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2447 mL | 11.2236 mL | 22.4472 mL |
| 5 mM | 0.4489 mL | 2.2447 mL | 4.4894 mL |
| 10 mM | 0.2245 mL | 1.1224 mL | 2.2447 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。