Opioid peptide manufacturer

Endomorphin-1

Agonist of μ-opioid receptors, highly potent and selective. Cas# 189388-22-5

Product Information

Catalog No. GP10065

Products are for research use only. Not for human use. We do not sell to patients.

Cas No.: 189388-22-5

Tel: (909) 407-4943 Email: admin@frankenthalerfoundation.org

Sample solution is provided at 25 µL, 10mM.

Protocol of Endomorphin-1

Cell experiment

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

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

• 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. Neuropharmacology, 1999, 38(2): 273-278.
• Tseng L F, Narita M, Suganuma C, et al. Differential antinociceptive effects of endomorphin-1 and endomorphin-2 in the mouse. Journal of Pharmacology and Experimental Therapeutics, 2000, 292(2): 576-583.
• Han Z, Jiang Y H, Wan Y, et al. Endomorphin-1 mediates 2 Hz but not 100 Hz electroacupuncture analgesia in the rat. Neuroscience letters, 1999, 274(2): 75-78.

Chemical Properties of Endomorphin-1

Cas No. 189388-22-5

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: C34 H38 N6 O5

Molecular Weight: 610.67

Solubility: ≥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.