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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.

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Opiorphin Chemical Structure

Opiorphin Chemical Structure

CAS No. : 864084-88-8

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Based on 1 publication(s) in Google Scholar

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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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

692.77

Formula

C29H48N12O8

CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

QRFSR

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (144.35 mM)

DMSO : 100 mg/mL (144.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4435 mL 7.2174 mL 14.4348 mL
5 mM 0.2887 mL 1.4435 mL 2.8870 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.83%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.4435 mL 7.2174 mL 14.4348 mL 36.0870 mL
5 mM 0.2887 mL 1.4435 mL 2.8870 mL 7.2174 mL
10 mM 0.1443 mL 0.7217 mL 1.4435 mL 3.6087 mL
15 mM 0.0962 mL 0.4812 mL 0.9623 mL 2.4058 mL
20 mM 0.0722 mL 0.3609 mL 0.7217 mL 1.8044 mL
25 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4435 mL
30 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2029 mL
40 mM 0.0361 mL 0.1804 mL 0.3609 mL 0.9022 mL
50 mM 0.0289 mL 0.1443 mL 0.2887 mL 0.7217 mL
60 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6015 mL
80 mM 0.0180 mL 0.0902 mL 0.1804 mL 0.4511 mL
100 mM 0.0144 mL 0.0722 mL 0.1443 mL 0.3609 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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