An NPFF receptor antagonist
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RF9

Item No. 31412

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-L-arginyl-L-phenylalaninamide
CAS Number
876310-60-0
Molecular Formula
C26H38N6O3
Formula Weight
482.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 5 mg/mlWater: 20 mg/ml
SMILES
O=C(C1(C[C@H](C2)C3)C[C@H]3C[C@H]2C1)N[C@@H](CCCNC(N)=N)C(N[C@H](C(N)=O)CC4=CC=CC=C4)=O
InChi Code
InChI=1S/C26H38N6O3/c27-22(33)21(12-16-5-2-1-3-6-16)31-23(34)20(7-4-8-30-25(28)29)32-24(35)26-13-17-9-18(14-26)11-19(10-17)15-26/h1-3,5-6,17-21H,4,7-15H2,(H2,27,33)(H,31,34)(H,32,35)(H4,28,29,30)/t17-,18+,19-,20-,21-,26?/m0/s1
InChi Key
UMKHUSRDQFQHAK-XIXLPFSXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $103

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    5 mg

    $378

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    10 mg

    $653

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    Product Description

    RF9 is a neuropeptide FF (NPFF) receptor antagonist.1 It 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Simonin, F., Schmitt, M., Laulin, J.-P., et al. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc. Natl. Acad. Sci. USA 103(2), 466-471 (2006).