Description
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
Product information
CAS Number: 1628843-99-1
Molecular Weight: 458.41
Formula: C22H18F4N6O
Chemical Name: (1S, 2R, 4R)-7-[3-fluoro-2-(pyrimidin-2-yl)benzoyl]-N-[5-(trifluoromethyl)pyrazin-2-yl]-7-azabicyclo[2.2.1]heptan-2-amine
Smiles: O=C(C1=CC=CC(F)=C1C1N=CC=CN=1)N1[C@H]2CC[C@@H]1C[C@H]2NC1=CN=C(C=N1)C(F)(F)F
InChiKey: NWUAUSABGZEYEW-WQVCFCJDSA-N
InChi: InChI=1S/C22H18F4N6O/c23-14-4-1-3-13(19(14)20-27-7-2-8-28-20)21(33)32-12-5-6-16(32)15(9-12)31-18-11-29-17(10-30-18)22(24,25)26/h1-4,7-8,10-12,15-16H,5-6,9H2,(H,30,31)/t12-,15-,16+/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and prolongs the time spent in REM sleep. JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses. JNJ-5471779 (5mg/kg; p.o.) shows low clearance.
Products are for research use only. Not for human use.
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