Opiorphin trifluoroacetate salt

Modify Date: 2024-01-09 01:48:28

Opiorphin trifluoroacetate salt Structure
Opiorphin trifluoroacetate salt structure
Common Name Opiorphin trifluoroacetate salt
CAS Number 864084-88-8 Molecular Weight 692.76700
Density N/A Boiling Point N/A
Molecular Formula C29H48N12O8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Opiorphin trifluoroacetate salt


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].

 Names

Name Opiorphin
Synonym More Synonyms

 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].
Related Catalog
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].
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.

 Chemical & Physical Properties

Molecular Formula C29H48N12O8
Molecular Weight 692.76700
Exact Mass 692.37200
PSA 366.84000
LogP 0.71060

 Synonyms

human opiorphin
H-Gln-Arg-Phe-Ser-Arg-OH