1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEndomorphin 1Cat. No.: HY-P0185CAS No.: 189388-22-5分式: CHNO分量: 610.7Sequence: Tyr-Pro-Trp-Phe-NH2Sequence Shortening: YPWF-NH2作靶點(diǎn): Opioid Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Protect from light, stored under nitro

2、genPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)現(xiàn)配，即刻使。溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 25 mg/mL (40.94 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6375 mL 8.1873 mL 16.3747 mL5 mM 0.3275 mL 1.6375 mL 3.2749 mL10 mM 0.1637 mL 0.8187 mL 1.6375 mL請(qǐng)根據(jù)產(chǎn)

3、品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Endomorphin 1，種度選擇性的親和-opioid受體激動(dòng)劑 ， 對(duì)kappa3結(jié)合位點(diǎn)具有親和 ，Ki為20 到 30 nM 之間。1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target Ki: 20-30 nM (kappa3 opioid receptor) 1體外研究 Endomorphin 1 (EM-1) is an endogenous opioid peptide and on

4、e of the two Endomorphins. It is a highaffinity, highly selective agonist of the -opioid receptor, and along with Endomorphin 2 (EM-2). The twoEndomorphins display reasonable affinities for kappa3 binding sites, with Ki values between 20 and 30 nM.Endomorphin 1 and Endomorphin 2 compete both 1 and 2

5、 receptor sites quite potently. Endomorphinshave little appreciable affinity for either delta or kappa1 binding sites, with Ki values greater than 500 nM 1.體內(nèi)研究 Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min,respectively. All subsequent studies are

6、 performed at peak effect. Both compounds are fully activesupraspinally and spinally, with no indication of ceiling effects. Endomorphin 1 is significantly more potentspinally than supraspinally and, at the spinal level, it is significantly more potent than Endomorphin 2. Theresponse of both agents

7、are readily reversed by naloxone. -FNA, a highly selective antagonist, effectivelyreverses the actions of both Endomorphins. Both Endomorphin 1 and Endomorphin 2 display a profile similarto morphine. Neither compound have analgesic activity in CXBK mice at a dose which produced over 70%analgesia in

8、control CD-1 mice 1.PROTOCOLKinase Assay 1 125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2 nM) is performed in potassium phosphate buffer (50mM, pH 7.4; 0.5 mL) with MgCl2 (5 mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06mg protein/mL for MOR-1/CHO cells. Specific bind

9、ing is determined in the presence and absence of either 1M of the corresponding unlabeled peptide. The entire mixture is then incubated at 25C for 1 hr and filteredover no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethylenimine and washed twicewith ice cold Tris buffer us

10、ing a Brandel cell harvester. The filters are then counted on a Packard Cobragamma counter. The other opioid receptor binding assays are performed 1 .MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Groups of mice are treate

11、d i.c.v. with Endomorphin 1 (12 g) or Endomorphin 2 (3 g) 15 min before a 0.5-cccharcoal meal (2.5% gum tragacanth,10% activated charcoal in water). The mice are killed 30 min later andthe distance the charcoal traveled is measured.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998Aug;286(2):1007-13.McePdfHeightCaution: Produc