Nerigliatin

Nerigliatin (PF-04937319) is a orally active glucokinase activator (GKA) with EC50 value of 154.4 μM. Nerigliatin maintains glucose-lowering efficacy. Nerigliatin causes peripheral nerve degeneration. Nerigliatin can be used in type 2 diabetes research.

Product Specifications

CAS Number

[1245603-92-2]

Product Name Alternative

PF-04937319

UNSPSC

12352005

Target

Glucokinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/nerigliatin.html

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=NC=C(OC2=C3C=C(C)OC3=CC(C(NC4=NC=C(C)N=C4)=O)=C2)C=N1)N(C)C

Molecular Formula

C22H20N6O4

Molecular Weight

432.43

References & Citations

[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.|[3]Sharma R, et al. Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator. Drug Metab Dispos. 2014 Nov;42 (11) :1926-39.|[4]Pettersen JC, et al. The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies. Toxicol Pathol. 2014 Jun;42 (4) :696-708.