Daridorexant hydrochloride is an orally active dual orexin type 1 and type 2 (OX1 and OX2) receptor antagonist (DORA) as well as an inhibitor of BCRP, with an IC50 value of 3.0 μM when acting on BCRP, and can be used in studies related to insomnia.
Molecular Weight | 487.39 |
Formula | C23H24Cl2N6O2 |
CAS Number | 1792993-84-0 |
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] No authors listed. Am J Health Syst Pharm. Daridorexant Hydrochloride
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