AR-M 1000390 hydrochloride

SKU: orb1222523

Description

AR-M 1000390 (hydrochloride), also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

Key Properties

• CAS Number: 209808-47-9
• MW: 384.94
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₉ClN₂O
• SMILES: Cl.CCN(CC)C(=O)c1ccc(cc1)\C(=C2/CCNCC2)c3ccccc3
• Target: δ-opioid receptor
• Solubility: DMSO : ≥ 150 mg/mL; 389.67 mM

Bioactivity

• In Vivo:
  Rats are treated with 5, 100, and 600 μmol/kg of AR-M 1000390 (AR-M100390) for 3 and/or 7 days; another group of rats treated with 600 μmol/kg of compound are allowed to recover for 14 days. AR-M 1000390 (600 μmol/kg) causes vacuolation in the β-cell of the rat pancreas that is associated with depletion of insulin and hyperglycemia after 7 days of dosing. Treatment of rats with 600 μmol/kg of AR-M 1000390 results in vacuolation of the β-cell of the rat pancreas that is similar to that reported for cyclizine and cyproheptadine.
• In Vitro:
  AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC50) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the μ receptor (IC50 = 3800±172 nM) and the κ receptor (IC50 = 7470±606 nM). RINm5F cells are treated with AR-M 1000390 (AR-M100390) and Cyclizine for 16-24 h before measurement of intracellular and secreted insulin levels. AR-M 1000390 mediates a dose-dependent decrease in insulin content with a maximal inhibition of ~90% at the highest concentration tested (10 μM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

δ-opioid receptor