中文名 | SRT 2104 |
英文名 | SRT 2104 |
别名 | 玻玛西林 化合物SRT2104 SRT 2104 选择性SIRT1活化剂 4-甲基-N-[2-[3-(吗啉基甲基)咪唑并[2,1-B]噻唑-6-基]苯基]-2-(吡啶-3-基)噻唑-5-甲酰胺 4-甲基-N-[2-[3-(4-吗啉基甲基)咪唑基[2,1-B]噻唑-6-基]苯基]-2-(3-吡啶基)-5-噻唑甲酰胺 |
英文别名 | CS-2293 SRT-2104 SRT 2104 GSK2245840 sirtuin Modulator SRT2104 (GSK2245840) (E)-3-(3-HYDROXY-4-METHOXYPHENYL)PROP-2-ENOIC ACID 4-Methyl-N-[2-[3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-(pyridin-3-yl)thiazole-5-carboxamide 5-ThiazolecarboxaMide, 4-Methyl-N-[2-[3-(4-MorpholinylMethyl)iMidazo[2,1-b]thiazol-6-yl]phenyl]-2-(3-pyridinyl)- |
CAS | 1093403-33-8 |
化学式 | C26H24N6O2S2 |
分子量 | 516.64 |
密度 | 1.46±0.1 g/cm3(Predicted) |
溶解度 | DMSO: 5毫克/毫升 (9.68毫米; 需要超声波) H2O : <0.1毫克/毫升 (不溶) |
酸度系数 | 11.40±0.70(Predicted) |
存储条件 | -20℃ |
体外研究 | SRT2104 reduces p65/RelA acetylation levels in C2C12 cells. SRT2104降低C2C12细胞中p65/RelA乙酰化水平。 |
体内研究 | In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, and enhances motor coordination, bone mineral density, and insulin sensitivity and decreased inflammation. Short-term SRT2104 treatment preserves bone and muscle mass in an experimental model of atrophy. In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival. 在雄性C57BL/6J小鼠体内,SRT2104 (100 mg/kg, p.o.)延长标准饮食喂养大鼠的平均和最大寿命,增强运动协调性,骨密度,和胰岛素敏感性,并减少炎症。在萎缩的实验模型中,短期SRT2104治疗保存骨头和肌肉质量。在雄性N171-82Q HD小鼠体内,SRT2104 (包含0.5% SRT2104的饮食)有效穿透血脑屏障,减弱脑萎缩,改善运动功能,并延长存活时间。 |
参考资料 展开查看 | 1: Baksi A, Kraydashenko O, Zalevkaya A, Stets R, Elliott P, Haddad J, Hoffmann E, Vlasuk GP, Jacobson EW. A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes. Br J Clin Pharmacol. 2014 Jul;78(1):69-77. doi: 10.1111/bcp.12327. PubMed PMID: 24446723; PubMed Central PMCID: PMC4168381. 2: van der Meer AJ, Scicluna BP, Moerland PD, Lin J, Jacobson EW, Vlasuk GP, van der Poll T. The Selective Sirtuin 1 Activator SRT2104 Reduces Endotoxin-Induced Cytokine Release and Coagulation Activation in Humans. Crit Care Med. 2015 Jun;43(6):e199-202. doi: 10.1097/CCM.0000000000000949. PubMed PMID: 25978169. 3: Sands BE, Joshi S, Haddad J, Freudenberg JM, Oommen DE, Hoffmann E, McCallum SW, Jacobson E. Assessing Colonic Exposure, Safety, and Clinical Activity of SRT2104, a Novel Oral SIRT1 Activator, in Patients with Mild to Moderate Ulcerative Colitis. Inflamm Bowel Dis. 2016 Mar;22(3):607-14. doi: 10.1097/MIB.0000000000000597. PubMed PMID: 26595549; PubMed Central PMCID: PMC4885523. 4: Venkatasubramanian S, Noh RM, Daga S, Langrish JP, Joshi NV, Mills NL, Hoffmann E, Jacobson EW, Vlasuk GP, Waterhouse BR, Lang NN, Newby DE. Cardiovascular effects of a novel SIRT1 activator, SRT2104, in otherwise healthy cigarette smokers. J Am Heart Assoc. 2013 Jun 14;2(3):e000042. doi: 10.1161/JAHA.113.000042. PubMed PMID: 23770971; PubMed Central PMCID: PMC3698759. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.936 ml | 9.678 ml | 19.356 ml |
5 mM | 0.387 ml | 1.936 ml | 3.871 ml |
10 mM | 0.194 ml | 0.968 ml | 1.936 ml |
5 mM | 0.039 ml | 0.194 ml | 0.387 ml |
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