SRT-2183
{{Drugbox | verifiedrevid = 477856488 | IUPAC_name = N-[2-(3-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}imidazo[2,1-b][1,3]thiazol-6-yl)phenyl]naphthalene-2-carboxamide | image = SRT2183 skeletal.svg
| tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = Investigational | routes_of_administration =
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =
| CAS_number_Ref = 
| CAS_number =
| ATC_prefix = None
| ATC_suffix =
| ChEMBL_Ref =
| ChEMBL = 403308
| PubChem = 24180126
| DrugBank_Ref =
| DrugBank =
| ChemSpiderID_Ref =
| ChemSpiderID = 23315224
| C=27 | H=24 | N=4 | O=2 | S=1
| molecular_weight = 468.570 g/mol
| smiles = c1ccc2cc(ccc2c1)C(=O)Nc3ccccc3c4cn5c(csc5n4)CN6CC[C@H](C6)O
| StdInChI_Ref =
| StdInChI = 1S/C27H24N4O2S/c32-22-11-12-30(15-22)14-21-17-34-27-29-25(16-31(21)27)23-7-3-4-8-24(23)28-26(33)20-10-9-18-5-1-2-6-19(18)13-20/h1-10,13,16-17,22,32H,11-12,14-15H2,(H,28,33)/t22-/m1/s1
| StdInChIKey_Ref =
| StdInChIKey = MUFSINOSQBMSLE-JOCHJYFZSA-N
}}
SRT2183 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 another SIRT1 activator SRT1720, but is closer in potency to resveratrol. 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 SRT2183 is a SIRT1 activator has been questioned[2] and further defended.[3]
See also
References
- ^ 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 (November 2007). "Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes". Nature. 450 (7170): 712–6. doi:10.1038/nature06261. PMC 2753457. PMID 18046409.
- ^ Pacholec M; Chrunyk BA; Cunningham D; Flynn D; Griffith DA; Griffor M; Loulakis P; Pabst B; Qiu X; Stockman B; Thanabal V; Varghese A; Ward J; Withka J; Ahn K (January 2010). "SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1". J Biol Chem. 285 (11): 8340–8351. doi:10.1074/jbc.M109.088682. PMC 2832984. PMID 20061378.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - ^ Dai H; Kustigian L; Carney D; Case A; Considine T; Hubbard BP; Perni RB; Riera TV; Szczepankiewicz B; Vlasuk GP; Stein RL (August 2010). "SIRT1 activation by small molecules - kinetic and biophysical evidence for direct interaction of enzyme and activator". J Biol Chem. 285 (43): 32695–32703. doi:10.1074/jbc.M110.133892. PMC 2963390. PMID 20702418.
{{cite journal}}: CS1 maint: unflagged free DOI (link)
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