Endomorphin-1, Inhibitor

Endomorphin-1

Cat. Num. AAA5764517

• Purity: 98.00%
• Synonyms: Endomorphin-1; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: Water: 24mg/mL (39.3mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C34H38N6O5
• SMILES: N[C@@H](Cc(cc1)ccc1O)C(N(CCC1)[C@@H]1C(N[C@@H](Cc1c[nH]c2c1cccc2)C(N[C@@H](Cc1ccccc1)C(N)=O)=O)=O)=O
• CAS Number: 189388-22-5
• Kinase Assay: 125I-Endomorphin 1 or 125I-Endomorphin 2 binding (0.2nM) is performed in potassium phosphate buffer (50mM, pH 7.4; 0.5 mL) with MgCl2 (5mM) at a tissue concentration of 10 mg wet weight/mL for brains or 0.06 mg protein/mL for MOR-1/CHO cells. Specific binding is determined in the presence and absence of either 1uM of the corresponding unlabeled peptide. The entire mixture is then incubated at 25 degree C for 1 hr and filtered over no. 32 glass fiber filters which have been presoaked for 1 hr in 0.5% polyethyleneimine and washed twice with ice-cold Tris buffer using a Brandel cell harvester. The filters are then counted on a Packard Cobra gamma counter. The other opioid receptor binding assays are performed.
• In Vitro: Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 minutes, respectively. All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound has analgesic activity in CXBK mice at a dose that produced over 70% analgesia in control CD-1 mice.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for Endomorphin-1, inhibitor

Endomorphin 1 is a high affinity and selective agonist of the u-opioid receptor and displays reasonable affinities for kappa3 binding sites (Ki: 20~30nM).

Product Categories/Family for Endomorphin-1, inhibitor

Endocrinology/Hormones; Opioid Receptor; Neuroscience

References

Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.