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PF 04937319,葡糖激酶部分激活剂

PF 04937319,葡糖激酶部分激活剂用途

PF-04937319 是一种葡萄糖激酶活化剂 (GKA),EC50 值为 154.4 μM,有望用来治疗 2 型糖尿病。PF-04937319 旨在维持降糖功效,同时降低许多其他 GKA 观察到的低血糖风险。

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PF 04937319,葡糖激酶部分激活剂名称

[ CAS 号 ]:
1245603-92-2

[ 中文名 ]:
PF 04937319,葡糖激酶部分激活剂

[ 英文名 ]:
PF 04937319

[英文别名 ]:

7E99B9ZM19
PF-04937319

PF 04937319,葡糖激酶部分激活剂生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 葡萄糖激酶

研究领域 >> 代谢疾病

[ 靶点 ]

EC50: 154.4 μM (GSA) (PF-04937319)[1]

[参考文献]

[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.

PF 04937319,葡糖激酶部分激活剂物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₂₂H₂₀N₆O₄

[ 分子量 ]:
432.432

[ 精确质量 ]:
432.154602

[ LogP ]:
1.29

[ 外观性状 ]:
粉末

[ 折射率 ]:
1.667

[ 储存条件 ]:
2-8°C，密封，干燥

PF 04937319,葡糖激酶部分激活剂安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

PF 04937319,葡糖激酶部分激活剂文献

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. 17(8) , 751-9, (2015)

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).Patie...

Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Drug Metab. Dispos. 42(11) , 1926-39, (2014)

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-ca...

The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies.

Toxicol. Pathol. 42(4) , 696-708, (2014)

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...

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