产品
编 号：F085177
分子式：C28H37N3O3S3
分子量：559.81
分子式：C28H37N3O3S3
分子量：559.81
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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50mg
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结构图
CAS No: 1234703-40-2
产品详情
生物活性：
Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucokinasein vitro: Globalagliatin activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.in vivo: Globalagliatin decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average Globalagliatin concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg Globalagliatin dose. The in vivo blood brain barrier permeability of Globalagliatin results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.
Globalagliatin (LY2608204) is a activator of glucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucokinasein vitro: Globalagliatin activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.in vivo: Globalagliatin decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average Globalagliatin concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg Globalagliatin dose. The in vivo blood brain barrier permeability of Globalagliatin results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.
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