1. Materials information
Names
Name | Opiorphin |
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Synonym | More Synonyms |
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Opiorphin trifluoroacetate salt Biological Activity
Description | 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]. |
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Related Catalog | Research Areas >> Neurological Disease Signaling Pathways >> Metabolic Enzyme/Protease >> Neprilysin |
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In Vitro | 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]. |
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In Vivo | 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]. Animal Model: Male Kunming mice[1] Dosage: 1.25, 2.5, 5, 10 μg/kg Administration: Intracerebroventrical injection; post-drug latency measurements were performed at 5, 10, 20, 30, 40, 50 and 60 min Result: Had the percentage change of tail withdrawal latency (TWL) at 10 min after i.c.v. administration of 1.25-10 mg/kg was 28.90%, 44.37%, 56.43% and 91.899.79%, respectively. |
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Chemical & Physical Properties
Molecular Formula | C29H48N12O8 |
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Molecular Weight | 692.76700 |
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Exact Mass | 692.37200 |
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PSA | 366.84000 |
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LogP | 0.71060 |
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MSDS
Opiorphin trifluoroacetate salt MSDS(Chinese) |
Synonyms
human opiorphin |
H-Gln-Arg-Phe-Ser-Arg-OH |
2. Packaging of materials
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