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Selisistat

Catalog No.: 52001
Cas No.: 49843-98-3
Purity : 98% Min.
52001 - Selisistat | CAS 49843-98-3

Catalog number : 52001

CAS number : 49843-98-3

分子式 : C13H13ClN2O

分子量 : 248.71

Iupac 化学名称 : 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

Smile : O=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N

InChiKey : FUZYTVDVLBBXDL-UHFFFAOYSA-N

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同义词EX-527; EX-527; EX-527; Selisistat
英文同义词EX-527; EX-527; EX-527; Selisistat
分子式C13H13ClN2O
分子量248.71
外观 类白色至白色固体
纯度98% Min.
可溶性可溶于DMSO;不溶于水
存储短期可在0-4度保存,数天至数月;长期可在-20度保存三年。
运输条件可在常温下运输
SmileO=C(C1C(NC2=C3C=C(Cl)C=C2)=C3CCC1)N
InChiKeyFUZYTVDVLBBXDL-UHFFFAOYSA-N
InChiInChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)
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Selisistat (6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide, SEN0014196, EX-527) is a selective SirT1 inhibitor that inhibits recombinant human SirT1 with an IC50 of 98 nm. It is more than 200-fold selective over SirT2 and SirT3 and has been shown to inhibit deacetylation of several SirT1 substrates both in vitro and in vivo. The compound exhibits cyto- and neuroprotective activity against toxicity induced by mutant HTT in cellular and in vivo models of HD increasing survival, amelioration of psychomotor behaviour and improvement in histopathological endpoints in the most widely employed animal models of HD. In a previous clinical study, selisistat was shown to be well tolerated at single doses up to 600 mg and repeated doses up to 300 mg day−1 for up to 7 days to healthy volunteers. The availability of selective, safe SirT1 inhibitors such as selisistat therefore makes the acetylation-dependent clearance of mutant HTT a clinically testable therapeutic approach.

[1]. Solomon JM, et al. Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage. Mol Cell Biol. 2006 Jan;26(1):28-38.

[2]. Jia Y, et al. SIRT1 is a regulator in high glucose-induced inflammatory response in RAW264.7 cells. PLoS One. 2015 Mar 20;10(3):e0120849.

[3]. Wang X, et al. Resveratrol attenuates microvascular inflammation in sepsis via SIRT-1-Induced modulation of adhesion molecules in ob/ob mice. Obesity (Silver Spring). 2015 Jun;23(6):1209-17.

[4]. Napper AD, et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. J Med Chem. 2005 Dec 15;48(25):8045-54.

[5]. Huang J, Tian R, Yang Y, Jiang R, Dai J, Tang L, Zhang L. The SIRT1 inhibitor EX-527 suppresses mTOR activation and alleviates acute lung injury in mice with endotoxiemia. Innate Immun. 2017 Nov;23(8):678-686. doi: 10.1177/1753425917733531. Epub 2017 Sep 27. 

[6].Tao YF, Lin F, Yan XY, Gao XG, Teng F, Fu ZR, Wang ZX. Galectin-9 in Combination With EX-527 Prolongs the Survival of Cardiac Allografts in Mice After Cardiac Transplantation. Transplant Proc. 2015 Jul-Aug;47(6):2003-9. doi: 10.1016/j.transproceed.2015.04.091. 

[7].Ohata Y, Matsukawa S, Moriyama Y, Michiue T, Morimoto K, Sato Y, Kuroda H. Sirtuin inhibitor Ex-527 causes neural tube defects, ventral edema formations, and gastrointestinal malformations in Xenopus laevis embryos. Dev Growth Differ. 2014 Aug;56(6):460-8. doi: 10.1111/dgd.12145. Epub 2014 Aug 5. 

[8]. Gertz M, Fischer F, Nguyen GT, Lakshminarasimhan M, Schutkowski M, Weyand M, Steegborn C. Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism. Proc Natl Acad Sci U S A. 2013 Jul 23;110(30):E2772-81. doi: 10.1073/pnas.1303628110. Epub 2013 Jul 9. 


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