JNJ-54717793 |
| Catalog No.GC63415 |
JNJ-54717793, como penetrante cerebral, es un antagonista del receptor de orexina-1 (OX1R) activo por vÍa oral, selectivo y de alta afinidad (EC50 plasmÁtico = 85 ng/mL).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628843-99-1
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
| Cas No. | 1628843-99-1 | SDF | |
| Formula | C22H18F4N6O | M.Wt | 458.41 |
| Solubility | DMSO : 240 mg/mL (523.55 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1815 mL | 10.9073 mL | 21.8145 mL |
| 5 mM | 436.3 μL | 2.1815 mL | 4.3629 mL |
| 10 mM | 218.1 μL | 1.0907 mL | 2.1815 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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