S85030 |
AS601245 |
源叶(MedMol) | 99% |
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- 产品描述: AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties
- 靶点: hJNK1:150 nM (IC50);hJNK2:220 nM (IC50);hJNK3:70 nM (IC50);JNK
- 体外研究:
AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells
- 体内研究:
AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia. AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice. Animal Model: C3H/HEN mice Dosage: 0.3, 1, 3, or 10 mg/kg Administration: P.o. Result: Decreased the TNF-α release in a dose-dependent manner.
- 参考文献:
1. Carboni S, et al. AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. J Pharmacol Exp Ther. 2004;310(1):25-32.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.685 ml 13.425 ml 26.85 ml 5 mM 0.537 ml 2.685 ml 5.37 ml 10 mM 0.268 ml 1.342 ml 2.685 ml 50 mM 0.054 ml 0.268 ml 0.537 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)