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Orexin receptor antagonist 3

Cat. No. M14037
Orexin receptor antagonist 3 Structure
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Biological Activity

Orexin receptor antagonist 3 (example 216) is an orexin receptor antagonist.

Chemical Information
Molecular Weight 434.45
CAS Number 1293282-55-9
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Catherine Roch, et al. Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia

[2] Becky X Lou, et al. Insomnia: Pharmacologic Treatment

[3] David C Earl, et al. New pharmacologic agents for insomnia and hypersomnia

[4] Yves Dauvilliers, et al. Daridorexant, a New Dual Orexin Receptor Antagonist to Treat Insomnia Disorder

[5] Patricia Murphy, et al. Lemborexant, A Dual Orexin Receptor Antagonist (DORA) for the Treatment of Insomnia Disorder: Results From a Bayesian, Adaptive, Randomized, Double-Blind, Placebo-Controlled Study

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