Opiorphin

立即咨询

Opiorphin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

864084-88-8

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

Opiorphin 是一种阿片类肽，是一种强效的人脑啡肽失活锌异肽酶抑制剂。Opiorphin 抑制两种脑啡肽分解外酶，人中性外肽内源性肽酶hNEP(EC 3.4.24.11)和人外氨基肽酶hAP-N(EC 3.4.11.2)。Opiorphin 通过激活内源性阿片依赖性传递显示出强大的镇痛活性。

生物活性

Opiorphin, an opioid peptide, is a potentenkephalin-inactivating zinc ectopeptidases in humaninhibitor. Opiorphin inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase,hNEP(EC 3.4.24.11) with anIC₅₀value 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].

体外研究
(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 IC₅₀value of 33 μM. and inhibits the Ala-pNA cleavage by hAP-N with an IC₅₀value of 65 μM^[2].

体内研究
(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.

分子量

692.77

Formula

C₂₉H₄₈N₁₂O₈

CAS 号

864084-88-8

Sequence Shortening

QRFSR

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.