| Bioactivity | 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. | ||||||||||||
| Name | Globalagliatin | ||||||||||||
| CAS | 1234703-40-2 | ||||||||||||
| Formula | C28H37N3O3S3 | ||||||||||||
| Molar Mass | 559.81 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Globalagliatin
CAS: 1234703-40-2 F: C28H37N3O3S3 W: 559.81
Globalagliatin (LY2608204) is a activator ofglucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucoki
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