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:
Molecular Weight:
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.
White to beige powder
PF-04991532; PF 04991532; PF04991532; PF-4991532; PF4991532; PF 4991532; UNII-AJ212MS2O2; CHEMBL2165620; AJ212MS2O2; SCHEMBL1711504; BDBM50394681; 6-[[(2S)-3-cyclopentyl-2-[4-(trifluoromethyl)imidazol-1-yl]propanoyl]amino]pyridine-3-carboxylic acid
Soluble in DMSO
-20°C Freezer
Type 2 diabetes mellitus
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Glucokinase Products

CAS 599164-57-5 RO 28-1674

RO 28-1674
(CAS: 599164-57-5)

RO 28-1674 is a glucokinase GK agonist.

CAS 866772-52-3 LBX192

(CAS: 866772-52-3)

LBX192 is a Liver Targeted Glucokinase Activator. It can activate the GK enzyme in vitro at low nM concentrations and reduce glucose levels during an oral gluco...

CAS 300353-13-3 Ro 28-1675

Ro 28-1675
(CAS: 300353-13-3)

A cell-permeable thiazolyl-propanamide compound that acts as a glucokinase (GK) activator by increasing Vmax and decreasing [S]1/2 of GK-catalyzed reaction as w...

CAS 1304015-76-6 ARRY 403

ARRY 403
(CAS: 1304015-76-6)

ARRY-403 is an orally available Glucokinase stimulants originated by Array BioPharma. ARRY-403 activates human glucokinase in vitro with EC50 of 79 nM at 5 mM g...

CAS 851884-87-2 GKA 50

GKA 50
(CAS: 851884-87-2)

GKA 50 is a potent glucokinase activator (EC50 = 33 nM). It causes a decrease in plasma glucose levels in diabetic rats and an increase of insulin release from ...

CAS 1234703-40-2 LY2608204

(CAS: 1234703-40-2)

LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations.

CAS 1215197-37-7 PF-04991532

(CAS: 1215197-37-7)

This active molecular is a hepatoselective glucokinase activator that reduces MDG (mean daily glucose), FPG (fasting plasma glucose) and glucose excursion in hu...

CAS 1442677-18-0 AM-9514

(CAS: 1442677-18-0)

AM-9514 is a glucokinase (GK) activator. It shows a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in...

Chemical Structure

CAS 1215197-37-7 PF-04991532

Quick Inquiry

Verification code

Featured Items