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Endomorphin-1

カタログ番号GP10065

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Endomorphin-1 化学構造

Cas No.: 189388-22-5

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$33.00
在庫あり
25mg
$36.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Protocol of Endomorphin-1

Cell experiment [1]:

Cell lines

Primary human fetal mixed glial/neuronal brain cell, human microglial cell

Preparation method

The solubility of this compound in DMSO is >30.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.1 nM

Applications

In mixed glial/neuronal cell cultures infected with HIV-1, endomorphin-1 potentiated the expression of HIV-1 in a bell-shaped dose-response manner. Endomorphin-1 (0.1 nM) consistently amplified the replication of HIV-1. In microglial cells, endomorphin-1 potentiated the expression of HIV-1, with maximal enhancement of HIV-1 expression at 10-10M.

Animal experiment [2, 3]:

Animal models

Male ICR mice, adult female Sprague–Dawley rats

Dosage form

i.c.v. injection, 5 min, 3.28 nM-16.38 nM, intrathecal injection

Application

Endomorphin-1 inhibited the tail-flick (AD50 = 6.16 nM) and hot-plate responses (AD50 = 1.94 nM) in a dose-dependent manner at 5 min after i.c.v. injection. In rats, intrathecal injection of 1:10 and 1:100 times diluted EM1 antiserum significantly decreased the effect of 2 Hz electroacupuncture analgesia.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Peterson P K, Gekker G, Hu S, et al. Endomorphin-1 potentiates HIV-1 expression in human brain cell cultures: implication of an atypical μ-opoid receptor[J]. Neuropharmacology, 1999, 38(2): 273-278.

[2]. Tseng L F, Narita M, Suganuma C, et al. Differential antinociceptive effects of endomorphin-1 and endomorphin-2 in the mouse[J]. Journal of Pharmacology and Experimental Therapeutics, 2000, 292(2): 576-583.

[3]. Han Z, Jiang Y H, Wan Y, et al. Endomorphin-1 mediates 2 Hz but not 100 Hz electroacupuncture analgesia in the rat[J]. Neuroscience letters, 1999, 274(2): 75-78.

Chemical Properties of Endomorphin-1

Cas No. 189388-22-5 SDF
Chemical Name (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
Canonical SMILES C1CC(N(C1)C(=O)C(CC2=CC=C(C=C2)O)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CC5=CC=CC=C5)C(=O)N
Formula C34H38N6O5 M.Wt 610.67
溶解度 ≥30.55mg/mL in DMSO Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Endomorphin-1

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.6375 mL 8.1877 mL 16.3755 mL
5 mM 0.3275 mL 1.6375 mL 3.2751 mL
10 mM 0.1638 mL 0.8188 mL 1.6375 mL
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計算

In vivo Formulation Calculator (Clear solution) of Endomorphin-1

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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