1. GPCR/G Protein
  2. Vasopressin Receptor

Fuscoside (Synonyms: OPC-21268)

Cat. No.: HY-15009 Purity: >98.0%
Handling Instructions

Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.

For research use only. We do not sell to patients.

Fuscoside Chemical Structure

Fuscoside Chemical Structure

CAS No. : 131631-89-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.

IC50 & Target

IC50: 0.4 μM (vasopressin V1)

Ki: 0.14 μM (vasopressin V1)[1]

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)[1].

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[1]. 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[2].

References
Animal Administration
[1]

Rats[1]

Male Sprague-Dawley rats, 300 to 400 g, are injected with Fuscoside (OPC-21268) (0.1, 0.3, 1 mg/kg). Fuscoside (OPC-21268) is given 2 min before the injection of AVP at 30 mU/kg i.v., angiotensin II at 0.3 μg/kg i.v., and noradrenaline at 3 μg/kg i.v.[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

449.54

Formula

C₂₆H₃₁N₃O₄

CAS No.

131631-89-5

SMILES

O=C(CC1)N(C2CCN(C(C3=CC=C(OCCCNC(C)=O)C=C3)=O)CC2)C4=C1C=CC=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Fuscoside
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Fuscoside

Cat. No.: HY-15009