ASP7663 is a selective TRPA1 activator (EC50 values are ~0.5 μM in human, mouse and rat). ASP7663 stimulates 5-HT release from QGP-1 cells.
ASP7663 exhibits an abdominal analgesic effect in vivo. ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide. ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat.
| Molecular Weight | 263.26 |
| Formula | C14H14FNO3 |
| CAS Number | 1190217-35-6 |
| Solubility (25°C) | DMSO 45 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.
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