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Purity: ≥98%
SRT2104 (formerly GSK-2245840; SRT2104; GSK2245840; SRT-2104) is a novel, first-in-class, brain penetrant, and highly selective small molecule activator of SIRT1 (Sirtuin 1) with potential use for neurodegenerative diseases. SIRT1 (Sirtuin 1) is involved in the regulation of energy homeostasis. Sirtuin 1 is a nicotinamide adenine dinucleotide-dependent protein deacetylase which regulates longevity and improves metabolism. Activation of Sirtuin 1 confers beneficial effects in models of neurodegenerative diseases. SRT2104 can penetrate the blood-brain barrier, attenuate brain atrophy, improve motor function, and extend survival in a mouse model of Huntington's disease. These findings imply a novel therapeutic strategy for Huntington's disease by targeting Sirtuin 1.
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| ln Vivo |
In diabetic mice, SRT 2104 (100 mg/kg/day, added to the diet for 24 weeks) raises SIRT1 protein without changing Sirt1 mRNA[2]. In diabetic mice, SRT 2104 (100 mg/kg/day, given in diet for 24 weeks) reduces oxidative stress in the testicles, apoptotic signaling activation, and endogenous stress[2]. In N171-82Q HD mice, SRT 2104 (0.5%; for 18 weeks) enhances motor function and increases survival[3].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/ 6 mice (8weeks old)[2]
Doses: 100 mg/kg/day Route of Administration: Supplemented in diet for 24 weeks Experimental Results: Enhanced SIRT1 protein without evelating Sirt1 mRNA level. Attenuated diabetes mellitus (DM)-induced oxidative stress, apoptotic signaling, and ER stress. Animal/Disease Models: WT and N171-82Q HD mice (6 weeks old)[3] Doses: 0.5% Route of Administration: 0.5% SRT 2104 containing diet for 6, 12, 18 weeks Experimental Results: Ameliorated motor deficits and increased survival in N171-82Q HD mice. |
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| References |
[1]. Hoffmann E, et al. Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man.
[2]. Jiao D, et al. MicroRNA-34a targets sirtuin 1 and leads to diabetes-induced testicular apoptotic cell death. J Mol Med (Berl). 2018 Sep;96(9):939-949. [3]. Jiang M, et al. Sirtuin 1 activator SRT2104 protects Huntington's disease mice. Ann Clin Transl Neurol. 2014 Dec;1(12):1047-52. |
| Molecular Formula |
C26H24N6O2S2
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| Molecular Weight |
516.64
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| CAS # |
1093403-33-8
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| Related CAS # |
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| SMILES |
O=C(C1=C(C)N=C(C2=CC=CN=C2)S1)NC3=CC=CC=C3C4=CN5C(SC=C5CN6CCOCC6)=N4
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| Chemical Name |
4-methyl-N-(2-(3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(pyridin-3-yl)thiazole-5-carboxamide
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| Synonyms |
GSK2245840; SRT2104; GSK-2245840; SRT 2104; GSK 2245840; SRT-2104.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01453491 | Completed | Drug: SRT2104 | Colitis, Ulcerative | Sirtris, a GSK Company | February 13, 2012 | Phase 1 |
| NCT01039909 | Withdrawn | Drug: Placebo Drug: SRT2104 |
Healthy Volunteer Atrophy, Muscular |
GlaxoSmithKline | January 2011 | Phase 1 |
| NCT01014117 | Completed | Drug: Placebo Drug: SRT2104 |
Sepsis | GlaxoSmithKline | December 9, 2009 | Phase 1 |
| NCT00937872 | Completed | Drug: 250 mg SRT2104 Suspension Drug: Carbon-14 radio-labeled SRT2104 |
Diabetes Mellitus, Type 2 | Sirtris, a GSK Company | November 22, 2008 | Phase 1 |
SRT2104 treatment improves whole-body physiology and extends lifespan in mice fed a standard diet.Aging Cell.2014 Oct;13(5):787-96. |
SRT2104 changes the gene expression profile differently in liver and muscle.Aging Cell.2014 Oct;13(5):787-96. |
SRT2104 treatment increases mitochondrial content and suppresses the inflammatory response.Aging Cell.2014 Oct;13(5):787-96. |
Short-term SRT2104 treatment preserves muscle and bone mass.Aging Cell.2014 Oct;13(5):787-96. |
SRT2104 ameliorated motor deficits and increased survival in N171-82Q HD mice.Ann Clin Transl Neurol.2014 Dec;1(12):1047-52. |
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