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OPC-51803

SKU: orb1699754

Description

OPC-51803 is a selective, orally active agonist of the vasopressin V2 receptor. It is utilized in research for conditions like nocturia and urinary incontinence, with studies demonstrating its effects in both in vitro receptor binding assays and in vivo models of diuresis.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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OPC-51803

Key Properties

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CAS Number192514-54-8
MW454
Purity98.93%
FormulaC26H32ClN3O2
SMILESC(=O)(N1C=2C([C@@H](CC(NC(C)C)=O)CCC1)=CC=CC2)C3=C(Cl)C=C(C=C3)N4CCCC4
TargetVasopressin Receptor
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (4.41 mM);DMSO:45 mg/mL (99.12 mM)

Bioactivity

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Target IC50
cAMP:189+/-14 nM(EC50)|V1a receptor:819+39 nM(Ki)|V2 receptor:91.9+10.8 nM(Ki)|V2 receptor:189+14 Nm(EC50)
In Vivo
OPC-51803 shows antidiuretic action in dogs. OPC-51803 (0.03 to 0.3 mg/kg; oral) decreased urine volume and increased urinary osmolality in a dose-dependent manner in water-loaded dogs. OPC-51803 infusions (0.3 and 3 microg x kg(-1) x min(-1); Intravenous ) did not affect renal or systemic hemodynamics in anesthetized dogs.
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In Vitro
OPC-51803 and dDAVP displaced [(3)H]-AVP binding to human V(2)- and V(1a)-receptors with K(i) values of 91.9+/-10.8 nM (n = 6) and 3.12+/-0.38 nM (n = 6) for V(2)-receptors, and 819+/-39 nM (n = 6) and 41.5+/-9.9 nM (n = 6) for V(1a)-receptors, indicating that OPC-51803 was about nine times more selective for V(2)-receptors, similar to the selectivity of dDAVP. OPC-51803 concentration-dependently increased cyclic adenosine 3', 5'-monophosphate (cyclic AMP) production in HeLa cells expressing human V(2)-receptors with an EC(50) value of 189+/-14 nM (n = 6).
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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OPC 51803, OPC51803, OPC-51803, SOU 003, SOU003, SOU-003, Vasopressin Receptor, vasopressin V1b receptor (AVPR1B), VasopressinReceptor

Similar Products

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  • (-)-OPC-51803

    (-)-OPC-51803 [orb1745241]

    99.59%

    192514-57-1

    454

    C26H32ClN3O2

    10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 1 mg, 5 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
3038506 ↗

Key Properties

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No computed properties available.

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OPC-51803 (orb1699754)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
¥ 3,640.00
5 mg
¥ 8,320.00
10 mg
¥ 13,000.00
25 mg
¥ 18,590.00
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