GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. In the intravenous glucose tolerance test, significant increases in the peak insulin response and insulin AUC (0-15 min) of 30-60% were reported in the GSK1292263 treatment group, compared with values in the vehicle control cohort. This insulin upregulation correlated with a significant increase in the glucose disposal rate.
|Animal models||male Sprague-Dawley rats|
|Formulation||0.9% sodium chloride solution|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 30 mg/mL|
|Source||Eur J Pharmacol (2017). Figure 2. GSK1292263|
|Incubation Time||0 to 4 h|
|Results||Our findings also demonstrated that all three GPR119 agonists (APD668, GSK1292263 and MBX2982) tested improved fat tolerance suggesting a GPR119 receptor mediated effect|
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