For research use only. Not for therapeutic Use.
Opiorphin, an opioid peptide, is a potent enkephalin-inactivating zinc ectopeptidases in human inhibitor. Opiorphin inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11) with an IC50 value of 11 μM, and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity by activating endogenous opioid-dependent transmission[1][2].
Opiorphin (1-100 μM; the mouse isolated colon) causes contractile effects in mouse distal colon in a concentration-dependent manner and enhances the contractile response induced by Met-enkephalin[1].
Opiorphin (0-50 μM; hNEP or hAP-N transformed HEK293 cell line) is a dual inhibitor of enkephalin-degrading hNEP and hAP-N in vitro. Opiorphin inhibits Mca-BK2 endoproteolysis by the cell-surface recombinant hNEP with an IC50 value of 33 μM. and inhibits the Ala-pNA cleavage by hAP-N with an IC50 value of 65 μM[2].
Opiorphin (1.25-10 μg/kg; ICV; 0-60 min; male Kunming mice) induces potent analgesic effect in a dose- and time-dependent manner (ED50=3.22 μg/kg)[1].
| Catalog Number | I042511 |
| CAS Number | 864084-88-8 |
| Synonyms | (2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]pentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]pentanoic acid |
| Molecular Formula | C29H48N12O8 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H48N12O8/c30-17(10-11-22(31)43)23(44)38-18(8-4-12-36-28(32)33)24(45)40-20(14-16-6-2-1-3-7-16)25(46)41-21(15-42)26(47)39-19(27(48)49)9-5-13-37-29(34)35/h1-3,6-7,17-21,42H,4-5,8-15,30H2,(H2,31,43)(H,38,44)(H,39,47)(H,40,45)(H,41,46)(H,48,49)(H4,32,33,36)(H4,34,35,37)/t17-,18-,19-,20-,21-/m0/s1 |
| InChIKey | TWWFCOBVAKAKIT-SXYSDOLCSA-N |
| SMILES | C1=CC=C(C=C1)CC(C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)O)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCC(=O)N)N |
| Reference | [1]. Tian XZ, et, al. Effects and underlying mechanisms of human opiorphin on colonic motility and nociception in mice. Peptides. 2009 Jul;30(7):1348-54. [2]. Wisner A, et, al. Human Opiorphin, a natural antinociceptive modulator of opioid-dependent pathways. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17979-84. |
