2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Endomorphin 1

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties.

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Endomorphin 1 Chemical Structure

Endomorphin 1 Chemical Structure

CAS No. : 189388-22-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 74 In-stock
Solution
10 mM * 1 mL in Water USD 74 In-stock
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5 mg USD 55 In-stock
10 mg USD 77 In-stock
25 mg USD 132 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Endomorphin 1:

Endomorphin 1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Endomorphin 1

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties[1][2][4].

IC50 & Target

μ Opioid Receptor/MOR

1.11 nM (Ki)

In Vitro

Endomorphin 1 inhibits Forskolin (HY-15371) (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells[5].
Endomorphin 1 (1-10 μM) increases interleukin-8 secretion in Caco-2 cells[6].
Endomorphin 1 (1 μM) inhibits excitatory transmission in adult rat substantia gelatinosa neurons[7].

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

Endomorphin 1 Related Antibodies
In Vivo

Endomorphin 1 (i.c.v.) shows antinociceptive properties in mice, with an ED50 value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v.) alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].

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

Animal Model: ICR mice[2].
Dosage: 6.16 nM (ED50)
Administration: Intracerebroventricularly (i.c.v.) injection
Result: Inhibited dose-dependently the tail-flick response.
Animal Model: Rats[3].
Dosage: 50 μg/kg
Administration: Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min.
Result: Alleviated MIRI by reducing the production of free radicals.
Dncreased LDH and CK-MB activities.
Increased SOD activity and decreased MDA content.
Decreased IL-6 and TNF-α plasma content.
Molecular Weight

610.70

Formula

C34H38N6O5
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Pro-Trp-Phe-NH2
Sequence Shortening

YPWF-NH2
Structure Classification
Initial Source
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: 

DMSO : ≥ 50 mg/mL (81.87 mM; 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 1.6375 mL 8.1873 mL 16.3747 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
DMSO 1 mM 1.6375 mL 8.1873 mL 16.3747 mL 40.9366 mL
5 mM 0.3275 mL 1.6375 mL 3.2749 mL 8.1873 mL
10 mM 0.1637 mL 0.8187 mL 1.6375 mL 4.0937 mL
15 mM 0.1092 mL 0.5458 mL 1.0916 mL 2.7291 mL
20 mM 0.0819 mL 0.4094 mL 0.8187 mL 2.0468 mL
25 mM 0.0655 mL 0.3275 mL 0.6550 mL 1.6375 mL
30 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3646 mL
40 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0234 mL
50 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
60 mM 0.0273 mL 0.1365 mL 0.2729 mL 0.6823 mL
80 mM 0.0205 mL 0.1023 mL 0.2047 mL 0.5117 mL
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Endomorphin 1 Related Classifications

Help & FAQs
  • 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.

Keywords:

Endomorphin 1189388-22-5Endomorphin1Endomorphin-1Opioid ReceptorAntinociceptionpaintail-flickMIRIischemia/reperfusion injuryCHOμ cellCaco-2Inhibitorinhibitorinhibit

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