产品
编 号：F486000
分子式：C29H48N12O8
分子量：692.77
分子式：C29H48N12O8
分子量：692.77
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 864084-88-8
产品详情
生物活性：
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.
体内研究：
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).Animal Model:Male Kunming mice
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.
体外研究：
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.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.
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.
体内研究：
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).Animal Model:Male Kunming mice
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.
体外研究：
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.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.
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