(S)-6-(3-Cyclopentyl-2-(4-(trifluoroMethyl)-1H-iMidazol- 1-yl)propanaMido)nicotinic Acid


CAS No. : 1215197-37-7

(S)-6-(3-Cyclopentyl-2-(4-(trifluoroMethyl)-1H-iMidazol- 1-yl)propanaMido)nicotinic Acid,1215197-37-7
Product Details
Cat No:M141433
Molecular Formula:C18H19F3N4O3
Molecular Weight:396.37
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Appearance:Solid powder
Purity: > 98%
Cat No:M141433
Cas No:1215197-37-7
Product-Name:(S)-6-(3-Cyclopentyl-2-(4-(trifluoroMethyl)-1H-iMidazol- 1-yl)propanaMido)nicotinic Acid
IUPAC Name:6-[[(2S)-3-cyclopentyl-2-[4-(trifluoromethyl)imidazol-1-yl]propanoyl]amino]pyridine-3-carboxylic acid
InChI:InChI=1S/C18H19F3N4O3/c19-18(20,21)14-9-25(10-23-14)13(7-11-3-1-2-4-11)16(26)24-15-6-5-12(8-22-15)17(27)28/h5-6,8-11,13H,1-4,7H2,(H,27,28)(H,22,24,26)/t13-/m0/s1
InChIKey:GKMLFBRLRVQVJO-ZDUSSCGKSA-N
SMILES:C1CCC(C1)CC(C(=O)NC2=NC=C(C=C2)C(=O)O)N3C=C(N=C3)C(F)(F)F
PF-04991532 is a potent and selective hepatoselective glucokinase activator. PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats. F-04991532 reduced plasma glucose concentrations independent of changes in insulin concentrations in a dose-dependent manner both acutely and after 28 days of sub-chronic treatment. PF-04991532 may offer glycemic control without inducing hepatic steatosis supporting the evaluation of tissue specific activators in clinical trials.

1: Sharma R, Litchfield J, Bergman A, Atkinson K, Kazierad D, Gustavson SM, Di L,
Pfefferkorn JA, Kalgutkar AS. Comparison of the circulating metabolite profile of
PF-04991532, a hepatoselective glucokinase activator, across preclinical species
and humans: potential implications in metabolites in safety testing assessment.
Drug Metab Dispos. 2015 Feb;43(2):190-8. doi: 10.1124/dmd.114.061218. Epub 2014
Nov 10. PubMed PMID: 25384899.
2: Ghosh A, Maurer TS, Litchfield J, Varma MV, Rotter C, Scialis R, Feng B, Tu M,
Guimaraes CR, Scott DO. Toward a unified model of passive drug permeation II: the
physiochemical determinants of unbound tissue distribution with applications to
the design of hepatoselective glucokinase activators. Drug Metab Dispos. 2014
Oct;42(10):1599-610. doi: 10.1124/dmd.114.058032. Epub 2014 Jul 14. PubMed PMID:
25024402.
3: Erion DM, Lapworth A, Amor PA, Bai G, Vera NB, Clark RW, Yan Q, Zhu Y, Ross
TT, Purkal J, Gorgoglione M, Zhang G, Bonato V, Baker L, Barucci N, D/'Aquila T,
Robertson A, Aiello RJ, Yan J, Trimmer J, Rolph TP, Pfefferkorn JA. The
hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia
without causing hepatic steatosis in diabetic rats. PLoS One. 2014 May
23;9(5):e97139. doi: 10.1371/journal.pone.0097139. eCollection 2014. PubMed PMID:
24858947; PubMed Central PMCID: PMC4032240.
4: Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen
J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens
BD, Bourassa P, D/'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F,
Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski
WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B,
Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J,
Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Discovery of
(S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotini
c acid as a hepatoselective glucokinase activator clinical candidate for treating
type 2 diabetes mellitus. J Med Chem. 2012 Feb 9;55(3):1318-33. doi:
10.1021/jm2014887. Epub 2012 Jan 24. PubMed PMID: 22196621.

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