PAT-1251 is a potent, selective, orally lysanyl oxidase-like protein 2 (LOXL2) inhibitor of hLOXL2 and hLOXL3 IC50 The values were 0.71 and 1.17 μM, respectively, and the inhibition of LOXL2 in mice, rats, and dogs was strong.IC50 Values are 0.10, 0.12, and 0.16 μM, respectively; PAT-1251 can be used for studies of a variety of fibrous diseases.
Molecular Weight | 399.34 |
Formula | C18H17F4N3O3 |
CAS Number | 2007885-39-2 |
Solubility (25°C) | DMSO ≥ 100 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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