| Revision as of 09:32, 20 February 2012 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Saving copy of the {{drugbox}} taken from revid 451605616 of page SRT2183 for the Chem/Drugbox validation project (updated: 'ChEMBL'). |
Latest revision as of 11:16, 25 May 2023 edit Mykhal (talk | contribs)Extended confirmed users5,566 edits added Category:Imidazothiazoles using HotCat |
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{{Short description|Organic compound, experimental pharmaceuticum}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Drugbox |
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{{Drugbox |
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| verifiedrevid = 477856488 |
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| Watchedfields = changed |
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| IUPAC_name = N-methyl}imidazothiazol-6-yl)phenyl]naphthalene-2-carboxamide |
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| verifiedrevid = 451167855 |
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| IUPAC_name = N-methyl}imidazothiazol-6-yl)phenyl]naphthalene-2-carboxamide |
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| image = SRT2183 skeletal.svg |
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| image = SRT2183 skeletal.svg |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V --> |
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| legal_status = Investigational |
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| legal_status = Investigational |
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| routes_of_administration = |
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| routes_of_administration = |
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<!--Pharmacokinetic data--> |
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<!--Pharmacokinetic data--> |
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| metabolism = |
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| metabolism = |
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| elimination_half-life = |
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| elimination_half-life = |
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| excretion = |
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| excretion = |
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<!--Identifiers--> |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = |
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| CAS_number = 1001908-89-9 |
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| ATC_prefix = None |
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| ATC_prefix = None |
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| ATC_suffix = |
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| ATC_suffix = |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 403308 |
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| ChEMBL = 403308 |
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| PubChem = 24180126 |
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| PubChem = 24180126 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 6FKU9G9CX6 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = |
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| DrugBank = |
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<!--Chemical data--> |
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<!--Chemical data--> |
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| C=27 | H=24 | N=4 | O=2 | S=1 |
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| C=27 | H=24 | N=4 | O=2 | S=1 |
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| molecular_weight = 468.570 g/mol |
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| smiles = c1ccc2cc(ccc2c1)C(=O)Nc3ccccc3c4cn5c(csc5n4)CN6CC(C6)O |
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| smiles = c1ccc2cc(ccc2c1)C(=O)Nc3ccccc3c4cn5c(csc5n4)CN6CC(C6)O |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = MUFSINOSQBMSLE-JOCHJYFZSA-N |
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| StdInChIKey = MUFSINOSQBMSLE-JOCHJYFZSA-N |
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}} |
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'''SRT-2183''' is a drug in development by ] intended as a ] ] of the ] subtype ]. It has similar activity in animal studies to another SIRT1 activator ], but is closer in potency to ]. In animal studies it was found to improve ] and lower ] levels in fat, muscle and liver tissue, and increased ] and ].<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> |
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However, the claim that SRT-2183 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> |
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== See also == |
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*] |
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== References == |
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{{Reflist}} |
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] |
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] |
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{{gastrointestinal-drug-stub}} |