MRE-269

SKU: orb1223120

Description

MRE-269, also known as ACT-333679, is a long-acting and highly selective prostacyclin receptor agonist. MRE-269, the active form or metabolite of Selexipag (NS-304), is much more selective for the IP receptor than are the prostacyclin analogs beraprost and iloprost, which also have high affinity for the EP(3) receptor.

Key Properties

• CAS Number: 475085-57-5
• MW: 419.52
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₉N₃O₃
• SMILES: CC1CCC2(CCC3(C(=CCC4C3(CCC5C4(CCC(=O)C5(C)C)C)C)C2C1C)C)C(=O)O
• Target: HIV-1 protease
• Solubility: DMSO : ≥ 50 mg/mL. 119.18 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  The vasorelaxant effects of MRE-269 on rat small intralobar pulmonary artery (SIPA) and EPA are the same, while the other IP receptor agonists induce less vasodilation in SIPA than in EPA. MRE-269 produces substantial relaxation of rat small pulmonary artery, although its effects are only significant at high concentrations of above 10 μM (pEC50, 4.98±0.22). By contrast, in rat small pulmonary veins, MRE-269 only produces minimal relaxation over the whole concentration range, with only significant relaxation occurring at the two highest doses of MRE-269 of 10 and 100 μM.
• In Vitro:
  MRE-269 induces endothelium-independent vasodilation of rat extralobar pulmonary artery (EPA). MRE-269 or other IP receptor agonists including epoprostenol, iloprost, treprostinil and beraprost increase cAMP levels in hPASMC. MRE-269 induces concentration-dependent vasodilation in LPA(+), LPA(-), and SPA(-).

Storage & Handling

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

Alternative Names

MRE-269 | MRE269 | MRE 269 | ACT-333679

Quick Database Links

Gene Symbol

HIV-1 protease