OPC 21268

SKU: orb1223346

Description

OPC-21268 is a vasopressin 1 receptor antagonist potentially for the treatment of heart failure and hypertension.(In Vitro):The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM).(In Vivo):Fuscoside (OPC-21268) competitively and specifically antagonizes pressor responses to AVP in vivo. Oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose- and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg. Fuscoside (OPC-21268) predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. Fuscoside (OPC-21268) treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages.

Key Properties

• CAS Number: 131631-89-5
• MW: 449.55
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₁N₃O₄
• SMILES: CC(=O)NCCCOC1=CC=C(C=C1)C(=O)N2CCC(CC2)N3C(=O)CCC4=CC=CC=C43
• Target: DNA/RNA Synthesis
• Solubility: DMSO : 50 mg/mL. 111.22 mM

Bioactivity

• In Vivo:
  Fuscoside (OPC-21268) competitively and specifically antagonizes pressor responses to AVP In vivo. Oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose-and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg. Fuscoside (OPC-21268) predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. Fuscoside (OPC-21268) treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages.
• In Vitro:
  The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM).

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

OPC-21268 | OPC21268 | OPC 21268

Quick Database Links

Gene Symbol

DNA/RNA Synthesis