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Nerigliatin

CAT: 0804-HY-108328-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-108328-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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.
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2