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| ln Vitro |
In Neuro 2A cells, RF9 (10 μM) pretreatment totally inhibited NPFF-induced neurite development [2].
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| ln Vivo |
Heroin-induced delayed hyperalgesia and tolerance are avoided when RF9 (0.1 mg/kg, subcutaneous injection) is administered concurrently with heroin [1]. MAP and heart rate did not alter significantly after receiving RF9 (10 μg) infusion alone. On the other hand, the NPFF-induced increases in heart rate and MAP are dramatically inhibited when RF9 is delivered in conjunction with NPFF [1].
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| Animal Protocol |
Animal/Disease Models: Rat[1].
Doses: 0.1 mg/kg. Route of Administration: 0.3 mg/kg heroin or saline was injected subcutaneously (sc) (sc) 30 minutes before basal nociceptive threshold in rats. Experimental Results: Against delayed heroin-induced hyperalgesia and related tolerance. |
| References |
[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.
[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. |
| Molecular Formula |
C26H38N6O3
|
|---|---|
| Molecular Weight |
482.63
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| Exact Mass |
482.3005
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| CAS # |
876310-60-0
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| Related CAS # |
RF9 hydrochloride
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
FC(C(=O)O[H])(F)F.O=C(C12C([H])([H])C3([H])C([H])([H])C([H])(C([H])([H])C([H])(C3([H])[H])C1([H])[H])C2([H])[H])N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[H])=O)C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H]
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| Synonyms |
RF-9 RF9 RF 9
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~259.00 mM)
H2O : ~16.67 mg/mL (~34.54 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (20.72 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0720 mL | 10.3599 mL | 20.7198 mL | |
| 5 mM | 0.4144 mL | 2.0720 mL | 4.1440 mL | |
| 10 mM | 0.2072 mL | 1.0360 mL | 2.0720 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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