PF 04937319,葡糖激酶部分激活剂

更新时间：2024-01-12 12:45:51

PF 04937319,葡糖激酶部分激活剂结构式	常用名	PF 04937319,葡糖激酶部分激活剂	英文名	PF 04937319
	CAS号	1245603-92-2	分子量	432.432
	密度	1.4±0.1 g/cm3	沸点	N/A
	分子式	C₂₂H₂₀N₆O₄	熔点	N/A
	MSDS	美版	闪点	N/A

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。

中文名	PF 04937319,葡糖激酶部分激活剂
英文名	7E99B9ZM19
英文别名	更多

描述	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。
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.

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

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

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...

2-Pyrimidinecarboxamide, N,N-dimethyl-5-[[2-methyl-6-[[(5-methyl-2-pyrazinyl)amino]carbonyl]-4-benzofuranyl]oxy]-

N,N-Dimethyl-5-({2-Methyl-6-[(5-Methylpyrazin-2-Yl)carbamoyl]-1-Benzofuran-4-Yl}oxy)pyrimidine-2-Carboxamide

7E99B9ZM19

N,N-Dimethyl-5-({2-methyl-6-[(5-methyl-2-pyrazinyl)carbamoyl]-1-benzofuran-4-yl}oxy)-2-pyrimidinecarboxamide

PF-04937319