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JNJ-54717793

Cat. No. M21270
JNJ-54717793  Structure
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Biological Activity

JNJ-54717793 is a selective octreotide-1 receptor antagonist used in studies of anxiety disorders, unlike the dual octreotide-1/2 inhibitors and octreotide-2 inhibitors typically used in sleep disorders.

Chemical Information
Molecular Weight 458.41
Formula C22H18F4N6O
CAS Number 1628843-99-1
Solubility (25°C) DMSO ≥ 200 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] Cathy Prville, et al. ACS Med Chem Lett. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793

[2] Pascal Bonaventure, et al. Front Pharmacol. Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation

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  Catalog
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