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YNT-185 

Cat. No. M28891
YNT-185  Structure
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Biological Activity

YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models.

Chemical Information
Molecular Weight 615.74
Formula C33H37N5O5S
CAS Number 1804978-81-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Eva Mezeiova, et al. Bioorg Chem. From orexin receptor agonist YNT-185 to novel antagonists with drug-like properties for the treatment of insomnia

[2] Yoko Irukayama-Tomobe, et al. Brain Nerve. [Development of a Therapeutic Drug for Narcolepsy]

[3] Shinichi Takenoshita, et al. Expert Opin Investig Drugs. An overview of hypocretin based therapy in narcolepsy

[4] Satoshi Toyama, et al. Anesthesiology. Nonpeptide Orexin-2 Receptor Agonist Attenuates Morphine-induced Sedative Effects in Rats

[5] Yoko Irukayama-Tomobe, et al. Proc Natl Acad Sci U S A. Nonpeptide orexin type-2 receptor agonist ameliorates narcolepsy-cataplexy symptoms in mouse models

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  Catalog
Abmole Inhibitor Catalog




Keywords: YNT-185  supplier, OX Receptor, inhibitors, activators


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