Endomorphin 1 acetate

SKU: orb1744910

Description

Endomorphin-1 acetate is a potent and selective μ-opioid receptor agonist with significant affinity for the kappa3 site. It is a valuable research tool for investigating pain mechanisms and analgesia in both in vitro binding assays and in vivo models of nociception.

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 (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.
• 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.

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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OpioidReceptor, Opioid Receptor, μ-opioid receptor

Compound Identifiers

PubChem CID

165437298