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- 产品描述: Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively.
- 靶点: JNK3:6 nM (IC50);JNK2:7 nM (IC50);JNK1:61 nM (IC50);JNK
- 体内研究:
Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis
- 参考文献:
1. Plantevin Krenitsky V, et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8. 2. Gan LT, et al. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Dec;61(6):1376-84. 3. Reich N, et al. Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis. Ann Rheum Dis. 2012 May;71(5):737-45. 4. Tavernier SJ, et al. Regulated IRE1-dependent mRNA decay sets the threshold for dendritic cell survival. Nat Cell Biol. 2017 Jun;19(6):698-710.
- 溶解性: Soluble in DMSO、1M HCl
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.23 ml 11.15 ml 22.3 ml 5 mM 0.446 ml 2.23 ml 4.46 ml 10 mM 0.223 ml 1.115 ml 2.23 ml 50 mM 0.045 ml 0.223 ml 0.446 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)