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.
|Related GPR Products|
NIBR189 is a small molecule antagonist of the Epstein-Barr virus-induced gene 2 (EBI2; GPR183) receptor with IC50 of 16 nM(Binding) and 11 nM (Functional).
Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure.
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of 7.62.
GSK137647A is a selective FFA4 agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively.
PSN375963 is a potent and selective agonist of GPR119 that shows similar potency to oleoyl ethanolamide (OEA) at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 8.4 and 7.9 µM, respectively (EC50 values for OEA are 3.2 and 2.9 µM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.