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Merck
모든 사진(1)

문서

PZ0320

Sigma-Aldrich

PF-04937319

≥98% (HPLC)

동의어(들):

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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모든 사진(1)

About This Item

실험식(Hill 표기법):
C22H20N6O4
CAS Number:
1245603-92-2
Molecular Weight:
432.43
MDL number:
MFCD26960571
UNSPSC 코드:
51111800
PubChem Substance ID:
329823838
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 20 mg/mL, clear

저장 온도

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

일반 설명

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

생화학적/생리학적 작용

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

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문서 라이브러리 방문

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
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

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