SRT-1460

SRT-1460
Identifiers

IUPAC name 3,4,5-trimethoxy-N-{2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl}benzamide
CAS Number	925432-73-1
PubChem CID	24180124
ChemSpider	23315250
CompTox Dashboard (EPA)	DTXSID40636044
Chemical and physical data
Formula	C₂₆H₂₉N₅O₄S
Molar mass	507.61 g·mol⁻¹
3D model (JSmol)	Interactive image
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 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 metabolic function.^[1] However, the claim that SRT1460 is a SIRT1 activator has been questioned^[2] and further defended.^[3]

References

^ Milne JC, Lambert PD, Schenk S, Carney DP, Smith JJ, Gagne DJ, et al. (November 2007). "Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes". Nature. 450 (7170): 712–6. Bibcode:2007Natur.450..712M. doi:10.1038/nature06261. PMC 2753457. PMID 18046409.
^ Pacholec M, Bleasdale JE, Chrunyk B, Cunningham D, Flynn D, Garofalo RS, et al. (March 2010). "SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1". The Journal of Biological Chemistry. 285 (11): 8340–51. doi:10.1074/jbc.M109.088682. PMC 2832984. PMID 20061378.
^ Dai H, Kustigian L, Carney D, Case A, Considine T, Hubbard BP, et al. (October 2010). "SIRT1 activation by small molecules: kinetic and biophysical evidence for direct interaction of enzyme and activator". The Journal of Biological Chemistry. 285 (43): 32695–703. doi:10.1074/jbc.M110.133892. PMC 2963390. PMID 20702418.

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This page was last edited on 24 July 2023, at 18:31