RF9
Based on 1 Customer Validation
RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.37%
- CAS. Nr.: 876310-60-0
- Formel: C26H38N6O3
- Molecular Weight:482.62
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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hNPFF1R 58 nM (Ki) |
hNPFF2R 75 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| COS-1 | EC50 |
379 nM
Compound: RF9, 1-Adamantanecarbonyl-RF-NH2
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Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
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[PMID: 22708927] |
| COS-1 | EC50 |
71 nM
Compound: RF9, 1-Adamantanecarbonyl-RF-NH2
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Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
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[PMID: 22708927] |
RF9 (10 μM) pretrement completely blocks NPFF induced neurite outgrowth of Neuro 2A cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RF9 (10 μg) infused alone does not result in a significant alteration of MAP or heart rate. Conversely, MAP and heart rate increases evoked by NPFF are significantly blocked when NPFF is applied in conjunction with RF9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1].
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Dosage:0.1 mg/kg.
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Administration:S.C. 30 min before 0.3 mg/kg heroin or saline on basal nociceptive threshold in rats.
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Result:Opposed to delaye heroin-induced hyperalgesia and associated tolerance.
Chemical Information
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CAS. Nr. 876310-60-0
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Appearance Solid
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Molecular Weight 482.62
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Formel C26H38N6O3
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Color White to off-white
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SMILES
NC([C@H](CC1=CC=CC=C1)NC([C@H](CCCNC(N)=N)NC(C23C[C@H](C4)C[C@H](C[C@H]4C3)C2)=O)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (207.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 16.67 mg/mL (34.54 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 10 mg/mL (20.72 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Simonin F, et al. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc Natl Acad Sci U S A. 2006 Jan 10;103(2):466-71. [Content Brief]
[2]. Ting Zhang, et al. Discovery of Two Novel Branched Peptidomimetics Containing endomorphin-2 and RF9 Pharmacophores: Synthesis and Neuropharmacological Evaluation. Bioorg Med Chem. 2019 Feb 15;27(4):630-643. [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 (sealed storage, away from moisture). 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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| H2O / DMSO | 1 mM | 2.0720 mL | 10.3601 mL | 20.7202 mL | 51.8006 mL |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | 10.3601 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL | 5.1801 mL | |
| 15 mM | 0.1381 mL | 0.6907 mL | 1.3813 mL | 3.4534 mL | |
| 20 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5900 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8288 mL | 2.0720 mL | |
| 30 mM | 0.0691 mL | 0.3453 mL | 0.6907 mL | 1.7267 mL | |
| DMSO | 40 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2950 mL |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0360 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3453 mL | 0.8633 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2590 mL | 0.6475 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5180 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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