product name LY2608204
Description: LY2608204 activates glucokinase (GK) with EC50 of 42 NM. LY2608204 has shown the novel and potent stimulant of glucokinase (GK) with the EC50 value of 42nM at lower glucose concentrations. In addition, LY2608204 has been reported to activate glucose metabolism with the EC50 value of 579nM in rat insulinoma INS1-E cell lines. Apart from these, LY2608204 has been revealed to lower plasma glucose in a dose-dependent fashion at the levels of fasted and postprandial.
References:
559.81
Formula
C28H37N3O3S3
CAS No.
1234703-40-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 112 mg/mL (200.1 mM)
Water: <1 mg/mL
Ethanol: 35 mg/mL (62.5 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 NM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | LY2608204 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 LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 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. |
| Animal model | Male Wistar rats at a weight of 225-250 g |
| Formulation & Dosage | Suspended in a 1:1 mixture of solutol/ethanol in a bath sonicator (10% of total volume). The obtained suspension is then diluted with 9 volumes of 10% aqueous solutol solution; 1, 3, 6, 10, 20 and 30 mg/kg; Orally, rats are given a 2 g/kg oral glucose bolus 2 hours after LY2608204 administration. |
| References |
