Endomorphin 1 acetate

Name: Endomorphin 1 acetate
Brand: MedChemExpress
SKU: HY-P0185A
Rating: 5.0 (2 reviews)

Cat. No.: HY-P0185A Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Endomorphin 1 acetate Chemical Structure

CAS No. : 1276123-71-7

Size	Price	Stock	Quantity
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Endomorphin 1 acetate:

Endomorphin 1 In-stock

2 Publications Citing Use of MCE Endomorphin 1 acetate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

μ Opioid Receptor/MOR

1.11 nM (Ki)

In Vitro

Endomorphin 1 acetate 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) acetate increases interleukin-8 secretion in Caco-2 cells^[6].
Endomorphin 1 (1 μM) acetate 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.

In Vivo

Endomorphin 1 (i.c.v.) acetate shows antinociceptive properties in mice, with an ED₅₀ value of 6.16 nM^[2].
Endomorphin 1 (50 μg/kg, i.v., rats) acetate 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

670.75

Formula

C₃₆H₄₂N₆O₇

CAS No.

1276123-71-7

Appearance

Solid

Color

White to off-white

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 : 125 mg/mL (186.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4909 mL	7.4543 mL	14.9087 mL
5 mM	0.2982 mL	1.4909 mL	2.9817 mL
10 mM	0.1491 mL	0.7454 mL	1.4909 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (284 KB) SDS (252 KB)

COA (257 KB) HNMR (343 KB) LCMS (250 KB)

Handling Instructions (2659 KB)

References

[1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13. [Content Brief]

[2]. Tseng LF. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Jpn J Pharmacol. 2002 Jul;89(3):216-20. [Content Brief]

[3]. Zhang WP, et al. Effects of endomorphin-1 postconditioning on myocardial ischemia/reperfusion injury and myocardial cell apoptosis in a rat model. Mol Med Rep. 2016 Oct;14(4):3992-8. [Content Brief]

[4]. Koda Y, et al. Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. Bioorg Med Chem. 2008 Jun 1;16(11):6286-96. [Content Brief]

[5]. Harrison C, et al. The effects of endomorphin-1 and endomorphin-2 in CHO cells expressing recombinant mu-opioid receptors and SH-SY5Y cells. Br J Pharmacol. 1999 Sep;128(2):472-8. [Content Brief]

[6]. Neudeck BL, et al. Endomorphin-1 alters interleukin-8 secretion in Caco-2 cells via a receptor mediated process. Immunol Lett. 2002 Dec 3;84(3):217-21. [Content Brief]

[7]. Fujita T, et al. Inhibition by endomorphin-1 and endomorphin-2 of excitatory transmission in adult rat substantia gelatinosa neurons. Neuroscience. 2006;139(3):1095-105. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4909 mL	7.4543 mL	14.9087 mL	37.2717 mL
	5 mM	0.2982 mL	1.4909 mL	2.9817 mL	7.4543 mL
	10 mM	0.1491 mL	0.7454 mL	1.4909 mL	3.7272 mL
	15 mM	0.0994 mL	0.4970 mL	0.9939 mL	2.4848 mL
	20 mM	0.0745 mL	0.3727 mL	0.7454 mL	1.8636 mL
	25 mM	0.0596 mL	0.2982 mL	0.5963 mL	1.4909 mL
	30 mM	0.0497 mL	0.2485 mL	0.4970 mL	1.2424 mL
	40 mM	0.0373 mL	0.1864 mL	0.3727 mL	0.9318 mL
	50 mM	0.0298 mL	0.1491 mL	0.2982 mL	0.7454 mL
	60 mM	0.0248 mL	0.1242 mL	0.2485 mL	0.6212 mL
	80 mM	0.0186 mL	0.0932 mL	0.1864 mL	0.4659 mL
	100 mM	0.0149 mL	0.0745 mL	0.1491 mL	0.3727 mL