Endomorphin 1 acetate

SKU: orb1744910

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.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1276123-71-7
• MW: 670.75
• Purity: 99.74%
• Formula: C₃₆H₄₂N₆O₇
• SMILES: C(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
• Target: Opioid Receptor
• Solubility: DMSO:100 mg/mL (149.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.96 mM)

Bioactivity

• Target IC50:
  μ opioid receptor:1.11 nM (Ki)
• In Vivo:
  Male Sprague Dawley rats ( = 8) were andomly divided into four groups ( = 2/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, subsequentl 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 wit the sham group. Compared wit 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 wit the sham group. Compared wit the IR group, IL-6, and TNF-α levels were significantly decreased in the IPO and Endomorphin 1 acetate groups.
• In Vitro:
  Caco-2 cells were treated with various concentration 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.

Storage & Handling

• Storage: keep 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.
• Disclaimer: For research use only

Alternative Names

OpioidReceptor, Opioid Receptor, μ-opioid receptor

Compound Identifiers

PubChem CID

165437298