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.
Molecular Weight | 505.50 |
Formula | C21H24FN7O5S |
CAS Number | 733750-99-7 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Related GPR/FFAR Products |
---|
[Ala17]-MCH
[Ala17]-MCH, a MCH analogue, is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). |
BigLEN(rat)
BigLEN(rat) is a potent GPR171 agonist with an EC50 of 1.6 nM. |
BigLEN(mouse)
BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. |
Neuropeptide EI, rat
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms. |
(Phe13, Tyr19)-MCH (human, mouse, rat)
(Phe13,Tyr19)-MCH (human, mouse, rat) is a potent SLC-1 and S643b receptor ligand. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.