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OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 332 € | In Stock | |
5 mg | 786 € | In Stock | |
10 mg | 1.073 € | In Stock | |
25 mg | 1.510 € | In Stock | |
50 mg | 1.881 € | In Stock | |
100 mg | 2.375 € | In Stock | |
500 mg | 4.655 € | In Stock |
Description | OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia. |
Targets&IC50 | V1a receptor:819+39 nM(Ki), V2 receptor:189+14 Nm(EC50), V2 receptor:91.9+10.8 nM(Ki), cAMP:189+/-14 nM(EC50) |
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.[5] 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).[5] |
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.[4] 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.[4] |
Alias | SOU-003, SOU003, SOU 003, OPC51803, OPC 51803 |
Molecular Weight | 454 |
Formula | C26H32ClN3O2 |
Cas No. | 192514-54-8 |
Smiles | C(=O)(N1C=2C([C@@H](CC(NC(C)C)=O)CCC1)=CC=CC2)C3=C(Cl)C=C(C=C3)N4CCCC4 |
Relative Density. | 1.31g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (99.12 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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