Porcupine-IN-1 is a potent porcupine inhibitor with IC50 value of 0.5±0.2 nM. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcupine-IN-1 potently inhibits the secretion of Wnt3A.
In vivo, Porcupine-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg).
| Molecular Weight | 410.44 |
| Formula | C25H19FN4O |
| CAS Number | 2036044-77-4 |
| Solubility (25°C) | DMSO ≥ 90 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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