View source for SRT-1460

{{short description|Chemical compound}}
{{Drugbox
| IUPAC_name = 3,4,5-trimethoxy-N-<nowiki/>{2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl}benzamide
| image = SRT-1460 structure.png
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B            / C / D / X -->
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
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<!--Identifiers-->
| CAS_number = 925432-73-1
| ATC_prefix =
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| PubChem = 24180124
| DrugBank =
| ChemSpiderID = 23315250
<!--Chemical data-->
| C=26 | H=29 | N=5 | O=4 | S=1
| smiles = COc1cc(cc(c1OC)OC)C(=O)Nc2ccccc2c3cn4c(csc4n3)CN5CCNCC5
}}
'''SRT-1460''' is a drug in development by [[Sirtris Pharmaceuticals]] intended as a [[small-molecule]] [[sirtuin activator|activator]] of the [[sirtuin]] subtype [[SIRT1]]. It has similar activity in animal studies to the known SIRT1 activator [[resveratrol]], but is closer in potency to [[SRT-1720]]. In animal studies it was found to improve [[insulin sensitivity]] and lower [[plasma glucose]] levels in fat, muscle and liver tissue, and increased [[mitochondrial]] and [[metabolism|metabolic function]].<ref name="pmid18046409">{{cite journal | vauthors = Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, Jin L, Boss O, Perni RB, Vu CB, Bemis JE, Xie R, Disch JS, Ng PY, Nunes JJ, Lynch AV, Yang H, Galonek H, Israelian K, Choy W, Iffland A, Lavu S, Medvedik O, Sinclair DA, Olefsky JM, Jirousek MR, Elliott PJ, Westphal CH | display-authors = 6 | title = Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes | journal = Nature | volume = 450 | issue = 7170 | pages = 712–6 | date = November 2007 | pmid = 18046409 | pmc = 2753457 | doi = 10.1038/nature06261 | bibcode = 2007Natur.450..712M }}</ref>
However, the claim that SRT1460 is a SIRT1 activator has been questioned<ref name="pmid20061378">{{cite journal | vauthors = Pacholec M, Bleasdale JE, Chrunyk B, Cunningham D, Flynn D, Garofalo RS, Griffith D, Griffor M, Loulakis P, Pabst B, Qiu X, Stockman B, Thanabal V, Varghese A, Ward J, Withka J, Ahn K | display-authors = 6 | title = SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1 | journal = The Journal of Biological Chemistry | volume = 285 | issue = 11 | pages = 8340–51 | date = March 2010 | pmid = 20061378 | pmc = 2832984 | doi = 10.1074/jbc.M109.088682 | doi-access = free }}</ref> and further defended.<ref name="pmid20702418">{{cite journal | vauthors = Dai H, Kustigian L, Carney D, Case A, Considine T, Hubbard BP, Perni RB, Riera TV, Szczepankiewicz B, Vlasuk GP, Stein RL | display-authors = 6 | title = SIRT1 activation by small molecules: kinetic and biophysical evidence for direct interaction of enzyme and activator | journal = The Journal of Biological Chemistry | volume = 285 | issue = 43 | pages = 32695–703 | date = October 2010 | pmid = 20702418 | pmc = 2963390 | doi = 10.1074/jbc.M110.133892 | doi-access = free }}</ref>
== See also ==
* [[SRT-2183]]
* [[STAC-9]]
== References ==
{{Reflist}}
[[Category:1-Piperazinyl compounds]]
[[Category:Imidazothiazoles]]
{{pharmacology-stub}}