SRT2104 (GSK2245840) |
Catalog No.GC15109 |
SRT2104 (GSK2245840) is a highly selective small-molecule activator of Sirtuin 1 (SIRT1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1093403-33-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
KGN, a human ovarian granulosa-like tumor cell line, derived from a granulosa cell tumors (GCT) patient |
Preparation Method |
The cells were seeded on cell culture dishes (5 × 105) and treated with EX 527 (50 µM) or SRT2104 (10 µM) for 24 h. Then, the cells were harvested and used for the SIRT Activity Assay Kit. |
Reaction Conditions |
10 µM, for 24 h |
Applications |
SRT2104 (GSK2245840) significantly increased SIRT1 deacetylation activity. |
Animal experiment [2]: | |
Animal models |
Male C57BL/6J mice |
Preparation Method |
For the longevity study, diets were started at 28 weeks of age after randomization into two groups of 100 mice per group. Mice were fed a standard AIN-93G diet (SD; carbohydrate:protein:fat ratio of 64:19:17 percent of kcal), or a SD supplemented with SRT2104. SRT2104 was added at a dose of 1.33 g drug per kg of chow, formulated to provide daily doses of ~ 100 mg drug kg-1 bodyweight. |
Dosage form |
100 mg kg-1 |
Applications |
SRT2104 supplementation resulted in improved survival of SD-fed mice with an increase in mean lifespan of 9.7% and in maximum lifespan (defined as the 10th percentile) of 4.9%. |
References: [1]: Schmid N, Dietrich KG, Forne I, Burges A, Szymanska M, Meidan R, Mayr D, Mayerhofer A. Sirtuin 1 and Sirtuin 3 in granulosa cell tumors. International Journal of Molecular Sciences. 2021 Feb 19;22(4):2047. |
SRT2104 (GSK2245840) is a highly selective small-molecule activator of Sirtuin 1 (SIRT1), penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and protected against diabetes-induced aortic endothelial dysfunction [1,2].
Treatment with SRT2104 (3μM, 48h) decreased P53 and Ac-P53 protein levels, but not P53 mRNA in HG-treated endothelial cells (ECs) [2]. Treatment with SRT2104 also (3μM, 48h) increased SIRT1 in protein level [2]. SRT2104 (10 μM, 24 h) significantly increased cell counts of KGN (an established cellular model for the majority of granulosa cell tumors (GCTs) and were used to explore the role of SIRT1), and SRT2104 significantly increased SIRT1 deacetylation activity [3].
SRT2104 (fed 0.5% with diet) improved motor function, increased survival, and attenuated brain atrophy in N171-82Q Huntington's disease (HD) mice [1]. SRT2104 (100 mg kg-1) treatment improves whole-body physiology and extends lifespan in mice fed a standard diet [4]. SRT2104-treated mice significantly reduced fasting blood glucose and insulin levels, and insulin resistance index [4]. SRT2104 (100 mg kg-1) treatment increases mitochondrial content and suppresses the inflammatory response [4]. SRT2104 alleviated muscle loss in hindlimb-unloading model in mice, and involutional and disuse-mediated osteoporosis [4]. SRT2104 improved diabetic nephropathy. SRT2104 (100 mg kg-1) protected diabetes mellitus (DM)-induced albuminuria and renal pathological injuries, and the was protective effect abrogated by P53 [5].
References:
[1]. Jiang M, Zheng J, Peng Q, Hou Z, Zhang J, Mori S, Ellis JL, Vlasuk GP, Fries H, Suri V, Duan W. Sirtuin 1 activator SRT 2104 protects Huntington's disease mice. Annals of clinical and translational neurology. 2014 Dec;1(12):1047-52.
[2]. Wu H, Wu J, Zhou S, Huang W, Li Y, Zhang H, Wang J, Jia Y. SRT2104 attenuates diabetes-induced aortic endothelial dysfunction via inhibition of P53. Journal of Endocrinology. 2018 Apr 1;237(1):1-4.
[3]. Schmid N, Dietrich KG, Forne I, Burges A, Szymanska M, Meidan R, Mayr D, Mayerhofer A. Sirtuin 1 and Sirtuin 3 in granulosa cell tumors. International Journal of Molecular Sciences. 2021 Feb 19;22(4):2047.
[4]. Mercken EM, Mitchell SJ, Martin?\Montalvo A, Minor RK, Almeida M, Gomes AP, Scheibye?\Knudsen M, Palacios HH, Licata JJ, Zhang Y, Becker KG. SRT 2104 extends survival of male mice on a standard diet and preserves bone and muscle mass. Aging cell. 2014 Oct;13(5):787-96.
[5]. Ma F, Wu J, Jiang Z, Huang W, Jia Y, Sun W, Wu H. P53/NRF2 mediates SIRT1's protective effect on diabetic nephropathy. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research. 2019 Aug 1;1866(8):1272-81.
Cas No. | 1093403-33-8 | SDF | |
Chemical Name | 4-methyl-N-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide | ||
Canonical SMILES | CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6 | ||
Formula | C26H24N6O2S2 | M.Wt | 516.64 |
Solubility | ≥ 6.46 mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.9356 mL | 9.6779 mL | 19.3558 mL |
5 mM | 0.3871 mL | 1.9356 mL | 3.8712 mL |
10 mM | 0.1936 mL | 0.9678 mL | 1.9356 mL |
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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