PF-04991532 - CAS 1215197-37-7
Catalog number: 1215197-37-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C18H19F3N4O3
Molecular Weight:
396.37
COA:
Inquire
Targets:
Glucokinase
Description:
This active molecular is a hepatoselective glucokinase activator that reduces MDG (mean daily glucose), FPG (fasting plasma glucose) and glucose excursion in humans. PF-04991532 may offer glycemic control without inducing hepatic steatosis. PF-04991532 was developed by Pfizer but was discontinued in Phase-II for Type-2 diabetes mellitus in USA in 2012.
Purity:
98%
Appearance:
White to beige powder
Synonyms:
UNII-AJ212MS2O2; CHEMBL2165620; AJ212MS2O2; SCHEMBL1711504; BDBM50394681; 6-[[(2S)-3-cyclopentyl-2-[4-(trifluoromethyl)imidazol-1-yl]propanoyl]amino]pyridine-3-carboxylic acid
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Type 2 diabetes mellitus
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
GKMLFBRLRVQVJO-ZDUSSCGKSA-N
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
Canonical SMILES:
C1CCC(C1)CC(C(=O)NC2=NC=C(C=C2)C(=O)O)N3C=C(N=C3)C(F)(F)F
Current Developer:
Originator: Pfizer
1.The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.
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 PLoS One. 2014 May 23;9(5):e97139. doi: 10.1371/journal.pone.0097139. eCollection 2014.
Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importance of glucose control. Glucokinase converts glucose to glucose-6-phosphate and determines glucose flux into the β-cells and hepatocytes. Since activation of glucokinase in β-cells is associated with increased risk of hypoglycemia, we hypothesized that selectively activating hepatic glucokinase would reduce fasting and postprandial glucose with minimal risk of hypoglycemia. Previous studies have shown that hepatic glucokinase overexpression is able to restore glucose homeostasis in diabetic models; however, these overexpression experiments have also revealed that excessive increases in hepatic glucokinase activity may also cause hepatosteatosis. Herein we sought to evaluate whether liver specific pharmacological activation of hepatic glucokinase is an effective strategy to reduce hyperglycemia without causing adverse hepatic lipids changes. To test this hypothesis, we evaluated a hepatoselective glucokinase activator, PF-04991532, in Goto-Kakizaki rats.
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Chemical Structure

CAS 1215197-37-7 PF-04991532

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