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AR-231453

Cat. No. M3766

AR-231453 Structure
Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 120 In stock
50mg USD 350 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 505.50
Formula C21H24FN7O5S
CAS Number 733750-99-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




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