1093403-33-8
SRT 2104
CAS: 1093403-33-8
Molecular Formula: C26H24N6O2S2
1093403-33-8 - Names and Identifiers
1093403-33-8 - Physico-chemical Properties
| Molecular Formula | C26H24N6O2S2 |
| Molar Mass | 516.64 |
| Density | 1.46±0.1 g/cm3(Predicted) |
| Solubility | DMSO : 5 mg/mL (9.68 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) |
| pKa | 11.40±0.70(Predicted) |
| Storage Condition | -20℃ |
| Use | SRT 2104 is a pioneering, highly selective Sirt1 (NAD-dependent) activator that can pass through the blood-brain barrier. It increases the level of Sirt1 protein, but has no effect on its mRNA. For the study of diabetes and Huntington's disease. |
| In vitro study | SRT2104 reduces p65/RelA levels in C2C12 cells. SRT2104 reduces the level of p65/RelA acetylation in C2C12 cells. |
| In vivo study | 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) effective expenses the blood-brain barrier, attributes brain atrophy, improve motor function, and extend survival. in male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) the average and maximum life span of rats fed the standard diet was prolonged, motor coordination, bone density, and insulin sensitivity were enhanced, and inflammation was reduced. 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 prolongs survival. |
1093403-33-8 - Reference
| Reference Show more | 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. |
1093403-33-8 - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
1093403-33-8 - Reference Information
| biological activity | SRT2104 (GSK2245840) is a selective SIRT1 activator that participates in the regulation of energy balance. Phase 2. SRT2104 (GSK2245840) is a selective SIRT1 activator, which participates in the regulation of energy balance. Phase 2. |
| in vitro study | SRT2104 reduces p65/RelA acetylation levels in C2C12 cells. SRT2104 decreased p65/RelA acetylation level in C2C12 cells. |
| in vivo study | in male c57bl/6j mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard die, 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. in male C57BL/6J mice, SRT2104 (100 mg/kg, P. o.) prolongs the average and maximum life span of rats fed a standard diet, enhances motor coordination, bone density, and insulin sensitivity, and reduces inflammation. Short-term SRT2104 therapy preserves bone and muscle mass in an experimental model of atrophy. In male N171-82Q HD mice, SRT2104 (a diet containing 0.5% SRT2104) effectively penetrated the blood-brain barrier, weakened brain atrophy, improved motor function, and prolonged survival. |
| target | TargetValue SIRT1 |
| Target | Value |
Last Update：2024-04-09 21:54:55
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Product Name: 4-Methyl-N-(2-(3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(pyridin-3-yl)thiazole-5-carboxamide Request for quotationCAS: 1093403-33-8
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