AS1269574 is a potent, orally active GPR119 agonist with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates the TRPA1 cation channel and stimulates glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induced pancreatic β cells to secrete glucose-dependent insulin only under high glucose conditions. AS1269574 has potential for type 2 diabetes research.
Molecular Weight | 308.17 |
Formula | C13H14BrN3O |
CAS Number | 330981-72-1 |
Form | Solid |
Solubility (25°C) | DMSO 30.82 mg/mL |
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.
[1] Ashcroft and Gribble. TiPS. New windows on the mechanism of action of KATP channel openers.
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