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MedKoo Cat#: 564411 | Name: RF9
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

RF9 is a potent and selective neuropeptide FF receptor antagonist, targeting both NPFF1 and NPFF2 receptors.

Chemical Structure

RF9
RF9
CAS#876310-60-0

Theoretical Analysis

MedKoo Cat#: 564411

Name: RF9

CAS#: 876310-60-0

Chemical Formula: C26H38N6O3

Exact Mass: 482.3005

Molecular Weight: 482.63

Elemental Analysis: C, 64.71; H, 7.94; N, 17.41; O, 9.94

Price and Availability

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1mg USD 370.00
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Synonym
RF-9; RF 9; RF9
IUPAC/Chemical Name
2-Adamantanecarbonyl-Arg-Phe-NH2; (1S,3S,5S,7S)-N-((S)-1-(((S)-1-Amino-1-oxo-3-phenylpropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)adamantane-2-carboxamide
InChi Key
ZLSDDXOZWMSRNZ-BFLAJNRSSA-N
InChi Code
InChI=1S/C26H38N6O3/c27-23(33)21(14-15-5-2-1-3-6-15)32-24(34)20(7-4-8-30-26(28)29)31-25(35)22-18-10-16-9-17(12-18)13-19(22)11-16/h1-3,5-6,16-22H,4,7-14H2,(H2,27,33)(H,31,35)(H,32,34)(H4,28,29,30)/t16?,17?,18?,19?,20-,21-,22?/m0/s1
SMILES Code
O=C(N[C@@H](CC1=CC=CC=C1)C(N)=O)[C@H](CCCNC(N)=N)NC(C2C3CC4CC(C3)CC2C4)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and water
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO and water
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
RF9 binds to human NPFF1 and NPFF2 receptors with Ki values of 58 and 75 nM, respectively. It is selective for NPFF1 and NPFF2 receptors over neuropeptide Y (NPY) receptor Y1, GPR10, GPR54, GPR103, ORL-1, and μ-, δ-, and κ-opioid receptors at 10 μM. RF9 (7.5 μM) inhibits NPFF-induced [35S]GTPγS binding to the NPFF2 receptor. It reverses NPVF-induced inhibition of forskolin-stimulated cAMP accumulation in CHO cells expressing the human NPFF1 receptor (EC50 = 4.7 μM). Intracerebroventricular administration of RF9 (10 μg) inhibits NPFF-induced increases in mean arterial pressure and heart rate in rats. It prevents heroin-induced delayed hyperalgesia and associated tolerance in rats when administered subcutaneously at a dose of 0.1 mg/kg.
In vitro activity:
To be determined
In vivo activity:
RF9 treatment significantly increased plasma testosterone levels in hydrocortisone treated intact adult male rhesus monkeys at 120 min (P ≤ 0.0037), 180 min (P ≤ 0.0016), and 240 min (P ≤ 0.0001) intervals. These results demonstrate that RF9 administration relieves the suppressed hypothalamic-pituitary-gonadal-axis in term of plasma testosterone levels in the cortisol treated monkeys. Reference: Front Physiol. 2021 Feb 25;12:630796. https://pubmed.ncbi.nlm.nih.gov/33716777/
Solvent mg/mL mM
Solubility
DMSO 5.0 10.36
Water 20.0 41.44
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 482.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Ullah R, Naz R, Batool A, Wazir M, Rahman TU, Nabi G, Wahab F, Fu J, Shahab M. RF9 Rescues Cortisol-Induced Repression of Testosterone Levels in Adult Male Macaques. Front Physiol. 2021 Feb 25;12:630796. doi: 10.3389/fphys.2021.630796. PMID: 33716777; PMCID: PMC7946976. 2. Simonin F, Schmitt M, Laulin JP, Laboureyras E, Jhamandas JH, MacTavish D, Matifas A, Mollereau C, Laurent P, Parmentier M, Kieffer BL, Bourguignon JJ, Simonnet G. 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. doi: 10.1073/pnas.0502090103. Epub 2006 Jan 3. Erratum in: Proc Natl Acad Sci U S A. 2006 Oct 24;103(43):16058. PMID: 16407169; PMCID: PMC1326150.
In vitro protocol:
To be determined
In vivo protocol:
1. Ullah R, Naz R, Batool A, Wazir M, Rahman TU, Nabi G, Wahab F, Fu J, Shahab M. RF9 Rescues Cortisol-Induced Repression of Testosterone Levels in Adult Male Macaques. Front Physiol. 2021 Feb 25;12:630796. doi: 10.3389/fphys.2021.630796. PMID: 33716777; PMCID: PMC7946976. 2. Simonin F, Schmitt M, Laulin JP, Laboureyras E, Jhamandas JH, MacTavish D, Matifas A, Mollereau C, Laurent P, Parmentier M, Kieffer BL, Bourguignon JJ, Simonnet G. 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. doi: 10.1073/pnas.0502090103. Epub 2006 Jan 3. Erratum in: Proc Natl Acad Sci U S A. 2006 Oct 24;103(43):16058. PMID: 16407169; PMCID: PMC1326150.
1: Ullah R, Batool A, Wazir M, Naz R, Rahman TU, Wahab F, Shahab M, Fu J. Gonadotropin inhibitory hormone and RF9 stimulate hypothalamic-pituitary-adrenal axis in adult male rhesus monkeys. Neuropeptides. 2017 Dec;66:1-7. doi: 10.1016/j.npep.2017.07.005. Epub 2017 Jul 25. PubMed PMID: 28757099. 2: Min L, Leon S, Li H, Pinilla L, Carroll RS, Tena-Sempere M, Kaiser UB. RF9 Acts as a KISS1R Agonist In Vivo and In Vitro. Endocrinology. 2015 Dec;156(12):4639-48. doi: 10.1210/en.2015-1635. Epub 2015 Sep 29. PubMed PMID: 26418326; PubMed Central PMCID: PMC4655216. 3: Sahin Z, Canpolat S, Ozcan M, Ozgocer T, Kelestimur H. Kisspeptin antagonist prevents RF9-induced reproductive changes in female rats. Reproduction. 2015 May;149(5):465-73. doi: 10.1530/REP-14-0683. Epub 2015 Feb 23. PubMed PMID: 25713426. 4: Liu X, Herbison AE. RF9 excitation of GnRH neurons is dependent upon Kiss1r in the adult male and female mouse. Endocrinology. 2014 Dec;155(12):4915-24. doi: 10.1210/en.2014-1517. Epub 2014 Oct 16. PubMed PMID: 25322463. 5: Maletínská L, Tichá A, Nagelová V, Spolcová A, Blechová M, Elbert T, Zelezná B. Neuropeptide FF analog RF9 is not an antagonist of NPFF receptor and decreases food intake in mice after its central and peripheral administration. Brain Res. 2013 Mar 1;1498:33-40. doi: 10.1016/j.brainres.2012.12.037. Epub 2013 Jan 3. Erratum in: Brain Res. 2013 Mar 29;1503:108. PubMed PMID: 23291266. 6: Caraty A, Blomenröhr M, Vogel GM, Lomet D, Briant C, Beltramo M. RF9 powerfully stimulates gonadotrophin secretion in the ewe: evidence for a seasonal threshold of sensitivity. J Neuroendocrinol. 2012 May;24(5):725-36. doi: 10.1111/j.1365-2826.2012.02283.x. PubMed PMID: 22283564. 7: Wang YQ, Wang SB, Ma JL, Guo J, Fang Q, Sun T, Zhuang Y, Wang R. Neuropeptide FF receptor antagonist, RF9, attenuates the fever induced by central injection of LPS in mice. Peptides. 2011 Apr;32(4):702-6. doi: 10.1016/j.peptides.2010.12.001. Epub 2010 Dec 16. PubMed PMID: 21167893. 8: Pineda R, Garcia-Galiano D, Sanchez-Garrido MA, Romero M, Ruiz-Pino F, Aguilar E, Dijcks FA, Blomenröhr M, Pinilla L, van Noort PI, Tena-Sempere M. Characterization of the potent gonadotropin-releasing activity of RF9, a selective antagonist of RF-amide-related peptides and neuropeptide FF receptors: physiological and pharmacological implications. Endocrinology. 2010 Apr;151(4):1902-13. doi: 10.1210/en.2009-1259. Epub 2010 Feb 16. PubMed PMID: 20160130. 9: 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. doi: 10.1016/j.regpep.2007.12.007. Epub 2008 Jan 11. PubMed PMID: 18276024. 10: Simonin F, Schmitt M, Laulin JP, Laboureyras E, Jhamandas JH, MacTavish D, Matifas A, Mollereau C, Laurent P, Parmentier M, Kieffer BL, Bourguignon JJ, Simonnet G. 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. Epub 2006 Jan 3. Erratum in: Proc Natl Acad Sci U S A. 2006 Oct 24;103(43):16058. PubMed PMID: 16407169; PubMed Central PMCID: PMC1326150.

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