Endomorphin 1

SKU: orb1296088

Description

Endomorphin 1

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 189388-22-5
• MW: 610.7
• Purity: 95.92%
• Formula: C₃₄H₃₈N₆O₅
• SMILES: N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
• Target: Opioid Receptor
• Solubility: DMSO:242.5 mg/mL (397.09 mM);H2O:24 mg/mL (39.3 mM)

Bioactivity

• Target IC50:
  κ3 opioid receptor:20-30 nM (Ki)|μ opioid receptor:1.11 nM (Ki)
• In Vivo:
  Both Endomorphin 1 and Endomorphin 2 are potent analgesics with peak effects seen at 10 and 15 min, respectively All subsequent studies are performed at peak effect. Both compounds are fully active supraspinally and spinally, with no indication of ceiling effects. Both Endomorphin 1 and Endomorphin 2 display a profile similar to morphine. Neither compound has analgesic activity in CXBK mice at a dose that produced over 70% analgesia in control CD-1 mice.
• In Vitro:
  Endomorphin is an endogenous opioid peptide and one o the two Endomorphins. It is a high affinity, a highly Selective agonist o the μ-opioid receptor, and along with Endomorphin 2. Endomorphin 1 and Endomorphin 2 compete for both μ1 and μ2 receptor sites quite potently. Endomorphins have a little appreciable affinity for either delta or kappa1 binding sites, with Ki Values greater than 500 nM.
• Animal Research:
  Groups of mice are treated i.c.v. With Endomorphin 1 (12 μg) or Endomorphin 2 (3 μg) 15 min before a 0.5-cc charcoal meal (2.5% gum tragacanth,10% activated charcoal in water) the mice are killed 30 min later an the distanc the charcoal traveled is measured.

Storage & Handling

• Storage: keep away from moisture | 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

Opioid Receptor, OpioidReceptor, inhibit, Inhibitor, Endomorphin1, Endomorphin-1, Endomorphin 1, μ-opioid receptor

Compound Identifiers

PubChem CID

5311080