PF-04937319

A glucokinase activator

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库存: 现货

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1mg

￥400.00

320.00

- +
5mg

￥1212.00

970.00

- +
10mg

￥0.00

0.00

- +
50mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

PF-04937319 is an activator of glucokinase (EC₅₀s = 174, 407, and 269 nM for the recombinant human, rat, and dog enzymes, respectively).¹ It increases glucose-induced insulin secretion in isolated rat islets when used at concentrations of 4 and 12 ?M.² PF-04937319 (3-100 mg/kg) reduces postprandial plasma glucose levels in rats.

1.Petterson, J.C., Litchfield, J., Neef, N., et al.The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studiesToxicol. Pathol.42(4)696-708(2014) 2.Pffefferkorn, J.A., Guzman-Perez, A., Oates, P.J., et al.Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitusMedchemcomm.2828-839(2011)