PF 04937319

Names

[ Name ]:
PF 04937319

[Synonym ]:
2-Pyrimidinecarboxamide, N,N-dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-
N,N-Dimethyl-5-({2-Methyl-6-[(5-Methylpyrazin-2-Yl)carbamoyl]-1-Benzofuran-4-Yl}oxy)pyrimidine-2-Carboxamide
7E99B9ZM19
N,N-Dimethyl-5-({2-methyl-6-[(5-methyl-2-pyrazinyl)carbamoyl]-1-benzofuran-4-yl}oxy)-2-pyrimidinecarboxamide
PF-04937319

Biological Activity

[Description]:

PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus[1].PF-04937319 is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs[2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase

Research Areas >> Metabolic Disease

[Target]

EC50: 154.4 μM (GSA) (PF-04937319)[1]

[References]

[1]. Dzyurkevich MS, et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci Rep. 2017 Nov 22;7(1):16072.

[2]. Amin NB, et al. Two dose-ranging studies with PF-04937319, a systemic partial activator of glucokinase, as add-on therapy to metformin in adults with type 2 diabetes. Diabetes Obes Metab. 2015 Aug;17(8):751-9.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₂₂H₂₀N₆O₄

[ Molecular Weight ]:
432.432

[ Exact Mass ]:
432.154602

[ LogP ]:
1.29

[ Index of Refraction ]:
1.667

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Two dose-ranging studies with PF-04937319, a systemic partial activator of glucokinase, as add-on therapy to metformin in adults with type 2 diabetes.

Diabetes Obes. Metab. 17(8) , 751-9, (2015)

To assess the efficacy and safety of a range of doses of a systemic, partial, glucokinase activator, PF-04937319, as add-on therapy to metformin, in patients with type 2 diabetes mellitus (T2DM).Patie...

Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Drug Metab. Dispos. 42(11) , 1926-39, (2014)

The present article summarizes Metabolites in Safety Testing (MIST) studies on a glucokinase activator, N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-ca...

The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies.

Toxicol. Pathol. 42(4) , 696-708, (2014)

Glucokinase activators (GKAs) are being developed for the treatment of type 2 diabetes. The toxicity of 4 GKAs (PF-04279405, PF-04651887, piragliatin, and PF-04937319) was assessed in mice, rats, dogs...