1093403-33-8 Usage
Biological Activity
srt2104 (gsk2245840) is a selective sirt1 activator involved in the regulation of energy homeostasis. sirt1, also known as nad-dependent deacetylase sirtuin-1, is a member of the sirtuin family of proteins.
in vitro
in c2c12 myoblasts stably transfected with small hairpin rna to knock-down sirt1, srt2104 increased ap activity, a marker for osteogenic differentiation. this effect was totally dependent on sirt1 expression [1].
in vivo
in male c57bl/6j mice, administration of srt2104 (100 mg/kg, p.o.) extended both mean and maximal lifespan of mice fed a standard diet, and enhanced bone mineral density, motor coordination, and insulin sensitivity and decreased inflammation. short-term srt2104 administration preserved bone and muscle mass in an experimental model of atrophy [1]. in male n171-82q hd mice with huntington's disease, srt2104 (diet containing 0.5% srt2104) effectively penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and extended survival [2].
references
[1]. mercken e m, mitchell s j, martin‐montalvo a, et al. srt2104 extends survival of male mice on a standard diet and preserves bone and muscle mass[j]. aging cell, 2014, 13(5): 787-796.[2]. jiang m, zheng j, peng q, et al. sirtuin 1 activator srt2104 protects huntington's disease mice[j]. annals of clinical and translational neurology, 2014, 1(12): 1047-1052.
Check Digit Verification of cas no
The CAS Registry Mumber 1093403-33-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,9,3,4,0 and 3 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1093403-33:
(9*1)+(8*0)+(7*9)+(6*3)+(5*4)+(4*0)+(3*3)+(2*3)+(1*3)=128
128 % 10 = 8
So 1093403-33-8 is a valid CAS Registry Number.
1093403-33-8Relevant articles and documents
The identification of the SIRT1 activator SRT2104 as a clinical candidate
Ng, Pui Yee,Bemis, Jean E.,Disch, Jeremy S.,Vu, Chi B.,Oalmann, Christopher J.,Lynch, Amy V.,Carney, David P.,Riera, Thomas V.,Song, Jeffrey,Smith, Jesse J.,Lavu, Siva,Tornblom, Angela,Duncan, Meghan,Yeager, Marie,Kriksciukaite, Kristina,Gupta, Akanksha,Suri, Vipin,Elliot, Peter J.,Milne, Jill C.,Nunes, Joseph J.,Jirousek, Michael R.,Vlasuk, George P.,Ellis, James L.,Perni, Robert B.
, p. 793 - 797 (2013/12/04)
We have identified SRT2104 (4) as the first direct synthetic SIRT1 activator clinical candidate. The compound was derived from the optimization of a previously described imidazo[1,2-b]thiazole scaffold. SRT2104 was selected as a development candidate based on a combination of biochemical activity and pharmacokinetic profile. The in vivo characteristics of SRT2104 were superior to those of analogues with similar activation profiles. The overall preclinical profile suggests that the compound has potential to provide therapeutic benefit in a clinical setting. 2013 Bentham Science Publishers.
SIRTUIN MODULATING IMIDAZOTHIAZOLE COMPOUNDS
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Page/Page column 71, (2009/01/23)
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
