RF 9 |
カタログ番号GC15469
One-Click Copy Product Info
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RF 9 は強力かつ選択的なニューロペプチド FF 受容体アンタゴニストであり、hNPFF1R および hNPFF2R の Ki 値はそれぞれ 58 および 75 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 876310-60-0
Sample solution is provided at 25 µL, 10mM.
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Ki: 58 nM for NPFF1; 75 nM for NPFF2
RF 9 is a neuropeptide FF receptors antagonist.
Neuropeptide FF (NPFF) has been isolated originally from bovine brain through its cross-reaction with antibodies to the molluscan cardioexcitory peptide FMRF-NH2, which possesses the similar C-terminal sequence. Recent studies shows that NPFF belongs to a neuropeptide family including two G protein-coupled receptors (NPFF1 and NPFF2) and two precursors (pro-NPFFA and pro-NPFFB). Both in vitro and in vivo studies have indicated that NPFF involves in a variety of biological actions.
In vitro: RF9 was found as a potent and selective NPFF receptor antagonist. RF9 was shown to be able to selectively bind to recombinant NPFF1 or NPFF2 receptors expressed in CHO or COS-1 cell and could also in vitro antagonize the agonism induced by NPFF and NPVF in the functional assays [1].
In vivo: Aminal in vivo study showed RF9 (30 nmol) injection failed to induce significant effect, but RF9 could completely antagonize the hypothermia of NPFF after cerebral administration in mice. Additionally, RF9 (30 nmol) co-injected in the third ventricle reduced the hypothermia induced by morphine or nociceptin/orphanin [2].
Clinical trial:N/A
References:
[1] Fang Q,Wang YQ,He F,Guo J,Guo J,Chen Q,Wang R. Inhibition of neuropeptide FF (NPFF)-induced hypothermia and anti-morphine analgesia by RF9, a new selective NPFF receptors antagonist. Regul Pept.2008 Apr 10;147(1-3):45-51.
[2] Wang YQ,Guo J,Wang SB,Fang Q,He F,Wang R. Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice. Peptides.2008 Jul;29(7):1183-90.
Animal experiment: | Rats: Rats (n=5) are catheterized for measurement of arterial blood pressure and receive an in-dwelling cannula into the lateral cerebral ventricle. Arterial blood pressure and heart rate are continuously monitored. NPFF (10 μg in 10 μL of saline) is injected into the lateral ventricle over 15 to 20 sec. Control injections of saline (10 μL) are carried out in the same animals. Upon return of blood pressure to baseline, RF9 (10 μg) is injected i.c.v., followed by another i.c.v. injection of NPFF with RF9. After 1.5 h., another i.c.v. infusion of NPFF is repeated[1]. |
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. | |
| Cas No. | 876310-60-0 | SDF | |
| Chemical Name | (3S,5S,7S,Z)-N-((S,Z)-5-guanidino-1-hydroxy-1-(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)pentan-2-yl)adamantane-1-carbimidic acid | ||
| Canonical SMILES | N=C(O)[C@](/N=C(O)/[C@](/N=C(O)/C12C[C@@]3([H])C[C@](C1)([H])C[C@](C2)([H])C3)([H])CCCNC(N)=N)([H])CC4=CC=CC=C4 | ||
| Formula | C26H38N6O3 | M.Wt | 482.62 |
| 溶解度 | DMSO: 5 mg/ml,Water: 20 mg/ml | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.072 mL | 10.3601 mL | 20.7202 mL |
| 5 mM | 414.4 μL | 2.072 mL | 4.144 mL |
| 10 mM | 207.2 μL | 1.036 mL | 2.072 mL |
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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 saline, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)