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AR-231453

Cat. No. M3766
AR-231453 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Chu ZL, et al. Mol Endocrinol. N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.

[2] Semple G, et al. J Med Chem. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.

[3] Chu ZL, et al. Endocrinology. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release.

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