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OPC-51803

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Catalog No. T28257Cas No. 192514-54-8
Alias SOU-003, SOU003, SOU 003, OPC51803, OPC 51803

OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.

OPC-51803

OPC-51803

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🥰Excellent
Purity: 98.93%
Catalog No. T28257Alias SOU-003, SOU003, SOU 003, OPC51803, OPC 51803Cas 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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$237In StockIn Stock
5 mg$593In StockIn Stock
10 mg$953In StockIn Stock
25 mg$1,390In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Batch Information

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Purity:98.93%
ee:99.06%
Appearance:Solid
Color:White
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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:91.9+10.8 nM(Ki), V2 receptor:189+14 Nm(EC50), V1a receptor:819+39 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]
SynonymsSOU-003, SOU003, SOU 003, OPC51803, OPC 51803
Chemical Properties
Molecular Weight454
FormulaC26H32ClN3O2
Cas No.192514-54-8
SmilesC(=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 & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (99.12 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.41 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

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