JNJ-10397049
Based on 1 publication(s) in Google Scholar
JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.
For research use only. We do not sell to patients.
- Purity: 99.19%
- CAS No.: 708275-58-5
- Formula: C19H20Br2N2O3
- Molecular Weight:484.18
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) JNJ-10397049
MoreAll Orexin Receptor (OX Receptor) Isoforms
More
Biological Activity
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OX2 Receptor |
JNJ-10397049 blocks ethanol self-administration, place preference and reinstatement[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[2].
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Dosage:10 mg/kg.
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Administration:Subcutaneous administration.
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Result:Induced a significant reduction in NREM sleep latency and an increase in NREM sleep duration during the first 2 h after administration relative to vehicle treatment.
Chemical Information
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CAS No. 708275-58-5
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Appearance Solid
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Molecular Weight 484.18
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Formula C19H20Br2N2O3
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Color White to off-white
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SMILES
BrC1=C(NC(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)=O)C=CC(Br)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
2024 May 17;21(1):131. PMID: 38760784
Solvent & Solubility
DMSO : 170 mg/mL (351.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 4.25 mg/mL (8.78 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 4.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Laura C McAtee, et al. Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9. [Content Brief]
[2]. Christine Dugovic, et al. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. [Content Brief]
[3]. Da-Thao Tran, et al. Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur J Pharmacol. 2011 Sep 30;667(1-3):120-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0653 mL | 10.3267 mL | 20.6535 mL | 51.6337 mL |
| 5 mM | 0.4131 mL | 2.0653 mL | 4.1307 mL | 10.3267 mL | |
| 10 mM | 0.2065 mL | 1.0327 mL | 2.0653 mL | 5.1634 mL | |
| 15 mM | 0.1377 mL | 0.6884 mL | 1.3769 mL | 3.4422 mL | |
| 20 mM | 0.1033 mL | 0.5163 mL | 1.0327 mL | 2.5817 mL | |
| 25 mM | 0.0826 mL | 0.4131 mL | 0.8261 mL | 2.0653 mL | |
| 30 mM | 0.0688 mL | 0.3442 mL | 0.6884 mL | 1.7211 mL | |
| 40 mM | 0.0516 mL | 0.2582 mL | 0.5163 mL | 1.2908 mL | |
| 50 mM | 0.0413 mL | 0.2065 mL | 0.4131 mL | 1.0327 mL | |
| 60 mM | 0.0344 mL | 0.1721 mL | 0.3442 mL | 0.8606 mL | |
| 80 mM | 0.0258 mL | 0.1291 mL | 0.2582 mL | 0.6454 mL | |
| 100 mM | 0.0207 mL | 0.1033 mL | 0.2065 mL | 0.5163 mL |
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