AR-231453 enhances glucose-induced insulin release. Antidiabetic activity. AR-231453 is Orally active in vivo. The GPR119-specific agonist AR231453 significantly increased cAMP accumulation and insulin release in both HIT-T15 cells and rodent islets. In both cases, loss of GPR119 rendered AR231453 inactive. AR231453 also enhanced glucose-dependent insulin release in vivo and improved oral glucose tolerance in wild-type mice but not in GPR119-deficient mice. Diabetic KK/A(y) mice were also highly responsive to AR231453.
|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.
N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Chu ZL, et al. Mol Endocrinol. 2010 Jan;24(1):161-70. PMID: 19901198.
Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.
Semple G, et al. J Med Chem. 2008 Sep 11;51(17):5172-5. PMID: 18698756.
A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release.
Chu ZL, et al. Endocrinology. 2007 Jun;148(6):2601-9. PMID: 17289847.
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