Ro 64-6198
Based on 1 publication(s) in Google Scholar
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.31%
- CAS. Nr.: 280783-56-4
- Formel: C26H31N3O
- Molecular Weight:401.54
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Ro 64-6198
MoreAlle Opioid Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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NOP Receptor/ORL1 |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
21 nM
Compound: Ro-646198
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Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
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[PMID: 22541041] |
Ro 64-6198 also produces rapid desensitization of the NOP receptor. In vitro studies shows that treatment with Ro 64-6198 results in a functional desensitization of the receptor, a loss in binding sites, and an apparent decrease in binding affinity. The desensitization produced by Ro 64-6198 is not reversed by acidic washes[1].
Ro 64-6198 does recruit both arrestin3 (EC50 of 0.912 μM) and arrestin2 (EC50 of 1.20 μM) to the NOP receptor in a concentration-dependent manner comparably with N/OFQ[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 280783-56-4
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Appearance Solid
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Molecular Weight 401.54
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Formel C26H31N3O
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Color White to yellow
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SMILES
O=C1NCN(C2=CC=CC=C2)C13CCN([C@H]4CC[C@]5([H])CCCC6=C5C4=CC=C6)CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
Cardiovascular and renal effects of novel nonpeptide nociceptin opioid peptide receptor agonists. [Abstract]2022 Jan;179(2):287-300. PMID: 34705263
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (124.52 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (6.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Reinheit & Dokumentation
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Data Sheet (281 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)
Verweise
[1]. Shoblock JR. The pharmacology of Ro 64-6198, a systemically active, nonpeptide NOP receptor (opiate receptor-like 1, ORL-1) agonist with diverse preclinical therapeutic activity. CNS Drug Rev. 2007 Spring;13(1):107-36. [Content Brief]
[2]. Chang SD, et al. Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198). ACS Chem Neurosci. 2015 Dec 16;6(12):1956-64. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4904 mL | 12.4521 mL | 24.9041 mL | 62.2603 mL |
| 5 mM | 0.4981 mL | 2.4904 mL | 4.9808 mL | 12.4521 mL | |
| 10 mM | 0.2490 mL | 1.2452 mL | 2.4904 mL | 6.2260 mL | |
| 15 mM | 0.1660 mL | 0.8301 mL | 1.6603 mL | 4.1507 mL | |
| 20 mM | 0.1245 mL | 0.6226 mL | 1.2452 mL | 3.1130 mL | |
| 25 mM | 0.0996 mL | 0.4981 mL | 0.9962 mL | 2.4904 mL | |
| 30 mM | 0.0830 mL | 0.4151 mL | 0.8301 mL | 2.0753 mL | |
| 40 mM | 0.0623 mL | 0.3113 mL | 0.6226 mL | 1.5565 mL | |
| 50 mM | 0.0498 mL | 0.2490 mL | 0.4981 mL | 1.2452 mL | |
| 60 mM | 0.0415 mL | 0.2075 mL | 0.4151 mL | 1.0377 mL | |
| 80 mM | 0.0311 mL | 0.1557 mL | 0.3113 mL | 0.7783 mL | |
| 100 mM | 0.0249 mL | 0.1245 mL | 0.2490 mL | 0.6226 mL |
Ro 64-6198 Related Classifications
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