SRT2104 (GSK2245840) |
| Katalog-Nr.GC15109 |
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.
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Cas No.: 1093403-33-8
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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