S80601 |
T0901317 |
源叶(MedMol) | 99% |
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- 产品描述: T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice
- 靶点: EC50: 20 nM (LXRα) and 5 μM (FXR) Ki: 132 nM (RORα) and 51 nM (RORγ);Apoptosis;FXR;LiverXReceptor;ROR
- 体内研究:
T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis. T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance.
- 参考文献:
1. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. 2. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. 3. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol P 4. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. 5. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. 6. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66.
- 溶解性: DMSO : 100 mg/mL (207.76 mM; Need ultrasonic)
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.078 ml 10.388 ml 20.776 ml 5 mM 0.416 ml 2.078 ml 4.155 ml 10 mM 0.208 ml 1.039 ml 2.078 ml 50 mM 0.042 ml 0.208 ml 0.416 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)