RF9 - Neuropeptide Y Receptor Antagonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERF9Cat. No.: HY-107382CAS No.: 876310-60-0分式: CHNO分量: 482.62作靶點: Neuropeptide Y Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 150 mg/mL (310

2、.80 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0720 mL 10.3601 mL 20.7202 mL5 mM 0.4144 mL 2.0720 mL 4.1440 mL10 mM 0.2072 mL 1.0360 mL 2.0720 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 RF9種有效且有選擇性的神經(jīng)肽FF受體 (Neuropeptide FF receptor)

3、 拮抗劑 ，對于 hNPFF1R 和 hNPFF2R的 Ki 值分別為 585 和 759 nM。IC50 & Target Ki: 585 nM (hNPFF1R), 759 nM (hNPFF2R) 1體內(nèi)研究RF9 (10 g) infused alone does not result in a significant alteration of MAP or heart rate. Conversely, MAPand heart rate increases evoked by NPFF are significantly blocked when NPFF is applied

4、in conjunction with1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemERF9 1. It is worthy to note that RF9 (30 nmol) significantly reduces the hypothermia induced by morphine (5nmol) 2.PROTOCOLAnimal Rats: Rats (n=5) are catheterized for measurement of arterial blood pressure and receive an in-dwellin

5、gAdministration 1 cannula into the lateral cerebral ventricle. Arterial blood pressure and heart rate are continuously monitored.NPFF (10 g in 10 L of saline) is injected into the lateral ventricle over 15 to 20 sec. Control injections ofsaline (10 L) are carried out in the same animals. Upon return

6、 of blood pressure to baseline, RF9 (10 g) isinjected i.c.v., followed by another i.c.v. injection of NPFF with RF9. After 1.5 h., another i.c.v. infusion ofNPFF is repeated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Simonin F, et al

7、. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated withhyperalgesia. Proc Natl Acad Sci U S A. 2006 Jan 10;103(2):466-71.2. Wang YQ, et al. Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice. Peptides. 2008Jul;29(7):1183-90.McePdfHeightCaution: Product has not been fully validated for medical applications.For research