Company Name: |
TargetMol Chemicals Inc.
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Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:JNJ-54717793 CAS:1628843-99-1 Purity:98% Package:10 mg;25 mg
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| Methanone, [3-fluoro-2-(2-pyrimidinyl)phenyl][(1S,2R,4R)-2-[[5-(trifluoromethyl)-2-pyrazinyl]amino]-7-azabicyclo[2.2.1]hept-7-yl]- Basic information |
| Methanone, [3-fluoro-2-(2-pyrimidinyl)phenyl][(1S,2R,4R)-2-[[5-(trifluoromethyl)-2-pyrazinyl]amino]-7-azabicyclo[2.2.1]hept-7-yl]- Chemical Properties |
Boiling point | 558.6±50.0 °C(Predicted) | density | 1.459±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO : 240 mg/mL (523.55 mM; Need ultrasonic) | pka | 1.35±0.10(Predicted) | form | Solid | color | Off-white to pink |
| Methanone, [3-fluoro-2-(2-pyrimidinyl)phenyl][(1S,2R,4R)-2-[[5-(trifluoromethyl)-2-pyrazinyl]amino]-7-azabicyclo[2.2.1]hept-7-yl]- Usage And Synthesis |
Biological Activity | 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[1][2].
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[2].JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses[2].JNJ-5471779 (5mg/kg; p.o.) shows low clearance[1]. | References | [1]. Préville C, et al. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793. ACS Med Chem Lett. 2020;11(10):2002-2009. Published 2020 Apr 27. [2]. Bonaventure P, et al. Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation. Front Pharmacol. 2017;8:357. Published 2017 Jun 9. |
| Methanone, [3-fluoro-2-(2-pyrimidinyl)phenyl][(1S,2R,4R)-2-[[5-(trifluoromethyl)-2-pyrazinyl]amino]-7-azabicyclo[2.2.1]hept-7-yl]- Preparation Products And Raw materials |
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