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OPC-51803

OPC-51803
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Purity:100%
ee:98.84%
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OPC-51803

Catalog No. T28257Cas No. 192514-54-8
OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.
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Pack SizePriceAvailabilityQuantity
1 mg$350In Stock
5 mg$828In Stock
10 mg$1,130In Stock
25 mg$1,590In Stock
50 mg$1,980In Stock
100 mg$2,500In Stock
500 mg$4,900In Stock
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Product Introduction

Bioactivity
Description
OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.
Targets&IC50
V2 receptor:189+14 Nm(EC50), V1a receptor:819+39 nM(Ki), cAMP:189+/-14 nM(EC50), V2 receptor:91.9+10.8 nM(Ki)
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]
AliasSOU-003, SOU 003, SOU003, OPC51803, OPC 51803
Chemical Properties
Molecular Weight454
FormulaC26H32ClN3O2
Cas No.192514-54-8
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2026 mL11.0132 mL22.0264 mL110.1322 mL
5 mM0.4405 mL2.2026 mL4.4053 mL22.0264 mL
10 mM0.2203 mL1.1013 mL2.2026 mL11.0132 mL
20 mM0.1101 mL0.5507 mL1.1013 mL5.5066 mL
50 mM0.0441 mL0.2203 mL0.4405 mL2.2026 mL

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