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Key Documents

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PZ0320

Sigma-Aldrich

PF-04937319

≥98% (HPLC)

Sinónimos:

N, N-Dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide, N,N-Dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-2-pyrimidinecarboxamide

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About This Item

Fórmula empírica (notación de Hill):
C22H20N6O4
Número de CAS:
1245603-92-2
Peso molecular:
432.43
MDL number:
MFCD26960571
UNSPSC Code:
51111800
PubChem Substance ID:
329823838
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

room temp

SMILES string

CC(O1)=CC2=C1C=C(C(NC3=NC=C(C)N=C3)=O)C=C2OC4=CN=C(C(N(C)C)=O)N=C4

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)

InChI key

MASKQITXHVYVFL-UHFFFAOYSA-N

General description

PF-04937319 is a partial activator of glycokinase (GK) enzyme.

Biochem/physiol Actions

PF-04937319 is a glucokinase activator with an EC50 value of 174 nM. PF-04937319 was found to improve glycemic control in adults with type 2 diabetes when used in conjunction with metformin.
PF-04937319, unlike other glucokinase activators, is capable of maintaining lower-glucose levels without it resulting in hypoglycemia. In type II diabetic patients where metformin treatment is inadequate, PF-04937319 is capable of maintaining glycemic control within the acceptable risk-benefit profile.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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N B Amin et al.
Diabetes, obesity & metabolism, 17(8), 751-759 (2015-04-18)
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). Patients were randomized to once-daily PF-04937319 doses of 10
John C Pettersen et al.
Toxicologic pathology, 42(4), 696-708 (2014-04-29)
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, and/or monkeys. GKAs were administered for 2 to 8 weeks. Standard
Raman Sharma et al.
Drug metabolism and disposition: the biological fate of chemicals, 42(11), 1926-1939 (2014-08-22)
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-carboxamide (PF-04937319), which is under development for the treatment of type 2 diametes mellitus. Metabolic profiling in rat, dog, and human hepatocytes revealed that PF-04937319 is

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