Fuscoside

SKU: orb1302923

Description

Fuscoside (OPC-21268) is a non-peptide, selective antagonist of the arginine vasopressin V1 receptor, exhibiting an IC50 of 0.4 µM. It is a research tool used in vitro and in vivo to study cardiovascular and renal physiology, including conditions like hypertension and heart failure.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 131631-89-5
• MW: 449.54
• Purity: 99.66%
• Formula: C₂₆H₃₁N₃O₄
• SMILES: CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2ccccc12
• Target: Vasopressin Receptor
• Solubility: Ethanol:11.24 mg/mL (25 mM);DMSO:60 mg/mL (133.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.45 mM)

Bioactivity

• Target IC50:
  V1 receptor(rat):25 nM|V1 receptor(human):8800 nM
• In Vivo:
  METHODS: OPC-21268 was injected intravenously into dogs and rats at doses of 0.3, 1.0, and 3.0 mg/kg to study its antagonistic effects on arginine vasopressin (AVP)-induced vasoconstrictor responses in spinally anesthetized dogs. RESULTS OPC-21268 produced a right-parallel shift of the AVP dose-response curve in a dose-dependent manner; doses of OPC-21268 were similar to those that inhibited AVP-induced vasoconstrictor responses in rats; OPC-21268 acted as a V1-AVP receptor antagonist in peripheral resistance vessels of dogs and rats.
• In Vitro:
  Fuscoside (OPC-21268) can replace 50% of the specific AVP binding concentration (IC50), including 0.4 μM for VI receptors and 100 μM for V2 receptors; at the same time, the inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors is 0.14 μM.

Storage & Handling

• Storage: 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

Fuscoside, Inhibitor, inhibit, OPC 21268, OPC21268, OPC-21268, VasopressinReceptor, Vasopressin Receptor, Vasopressin receptor 1

Compound Identifiers

PubChem CID

114904