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Endomorphin 1 acetate

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Catalog No. T72423Cas No. 1276123-71-7

Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.

Endomorphin 1 acetate

Endomorphin 1 acetate

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Purity: 99.74%
Catalog No. T72423Cas No. 1276123-71-7
Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30-In Stock
5 mg$44-In Stock
10 mg$62-In Stock
25 mg$108-In Stock
50 mg$158-In Stock
100 mg$235-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.74%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.
Targets&IC50
μ opioid receptor:1.11 nM (Ki)
In vitro
Caco-2 cells were treated with various concentrations of Endomorphin 1 acetate. When cells were incubated with Endomorphin 1 acetate alone, no changes in basal IL-8 production were detected. However, treatment of Caco-2 cells with Endomorphin 1 acetate in the presence of IL-1β significantly increased IL-8 compared with cells treated with IL-1β alone. [1]
In vivo
Male Sprague Dawley rats (n=48) were randomly divided into four groups (n=12/group): i) Sham group, LAD ligation with no other intervention for 150 min; ii) IR group: LAD was ligated for 30 min (ischemia), and was reperfused for 120 min in vivo; iii) IPO group, after 30 min ischemia, three cycles of LAD clamping for 15 sec and declamping for 15 sec were performed before reperfusion; iv) EM50 group: Endomorphin 1 acetate (50 μg/kg) was administered intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min in vivo.
In the IR, IPO and Endomorphin 1 acetate groups, LDH and CK-MB activities were significantly higher compared with the sham group. Compared with the IR group, LDH and CK-MB activities were significantly decreased in the IPO and Endomorphin 1 acetate groups. In the IR group, IL-6 and TNF-α levels were significantly increased compared with the sham group. Compared with the IR group, IL-6, and TNF-α levels were significantly decreased in the IPO and Endomorphin 1 acetate groups. [2]
Chemical Properties
Molecular Weight670.75
FormulaC36H42N6O7
Cas No.1276123-71-7
SmilesC(C)(O)=O.C([C@H](NC(=O)[C@H]1N(C([C@H](CC2=CC=C(O)C=C2)N)=O)CCC1)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)C=4C=5C(NC4)=CC=CC5
SequenceH-Tyr-Pro-Trp-Phe-NH2.CH3CO2H
Sequence ShortYPWF
Storage & Solubility Information
Storagekeep away from moisture,store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 100 mg/mL (149.09 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (5.96 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.4909 mL7.4543 mL14.9087 mL74.5434 mL
5 mM0.2982 mL1.4909 mL2.9817 mL14.9087 mL
10 mM0.1491 mL0.7454 mL1.4909 mL7.4543 mL
20 mM0.0745 mL0.3727 mL0.7454 mL3.7272 mL
50 mM0.0298 mL0.1491 mL0.2982 mL1.4909 mL
100 mM0.0149 mL0.0745 mL0.1491 mL0.7454 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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