WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H522488
CAS#: 1245603-92-2
Description: PF-04937319 is a glucokinase activator which is under development for the treatment of type 2 diametes mellitus. Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells.
Hodoodo Cat#: H522488
Name: PF-04937319
CAS#: 1245603-92-2
Chemical Formula: C22H20N6O4
Exact Mass: 432.15
Molecular Weight: 432.440
Elemental Analysis: C, 61.10; H, 4.66; N, 19.43; O, 14.80
Synonym: PF-04937319; PF04937319; PF 04937319; PF-4937319; PF 4937319; PF4937319, nerigliatin
IUPAC/Chemical Name: N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide
InChi Key: MASKQITXHVYVFL-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H20N6O4/c1-12-8-24-19(11-23-12)27-21(29)14-6-17-16(5-13(2)31-17)18(7-14)32-15-9-25-20(26-10-15)22(30)28(3)4/h5-11H,1-4H3,(H,24,27,29)
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 432.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Amin NB, Aggarwal N, Pall D, Paragh G, Denney WS, Le V, Riggs M, Calle RA. 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. doi: 10.1111/dom.12474. Epub 2015 May
11. PubMed PMID: 25885172.
2: Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC,
Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS. 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. doi:
10.1124/dmd.114.060087. Epub 2014 Aug 20. PubMed PMID: 25142735.
3: Pettersen JC, Litchfield J, Neef N, Schmidt SP, Shirai N, Walters KM, Enerson
BE, Chatman LA, Pfefferkorn JA. 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. doi:
10.1177/0192623314526006. Epub 2014 Apr 24. PubMed PMID: 24771080.
