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PD-168077 maleate

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Catalog No. T5047Cas No. 630117-19-0

PD-168077 maleate is a selective agonist of the dopamine D4 receptor (Ki: 9 nM).

PD-168077 maleate

PD-168077 maleate

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Purity: 99.13%
Catalog No. T5047Cas No. 630117-19-0
PD-168077 maleate is a selective agonist of the dopamine D4 receptor (Ki: 9 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$48In StockIn Stock
10 mg$73In StockIn Stock
25 mg$153In StockIn Stock
50 mg$257In StockIn Stock
100 mg$383In StockIn Stock
200 mg$545-In Stock
1 mL x 10 mM (in DMSO)$53In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.13%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
PD-168077 maleate is a selective agonist of the dopamine D4 receptor (Ki: 9 nM).
Targets&IC50
D4:9 nM(Ki)
In vivo
PD-168077, a selective D4 dopamine receptor agonist, injected into the paraventricular nucleus of the hypothalamus on penile erection was studied in male rats.?PD-168077 (1-200 ng) induced penile erection in a dose-dependent manner.?The minimal effective dose was 50 ng, while the maximal response was found with 200 ng of the compound, which increased penile erection episodes from 0.3+/-0.03 to 1.7+/-0.21.?The proerectile effect of PD-168077 was reduced almost completely by L-745,870 (3-(4-[chlorophenyl]piperazin-1-yl)-methyl-1H-pyrrolo[2,3-B]pyridine trihydrochloride), a selective D4 dopamine receptor antagonist, (1 microg) given into the paraventricular nucleus before the D4 dopamine agonist, and by other nonselective dopamine receptor antagonists, such as haloperidol (1 microg) and clozapine (1 microg), which block all dopamine receptor subtypes.?The pro-erectile effect of PD-168077 was also reduced by the NO synthase inhibitor NG-nitro-L-arginine methylester (25 microg), but not by the oxytocin receptor antagonist d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg), when given into the paraventricular nucleus.?In spite of its inability to prevent the pro-erectile effect of PD-168077 when given in the paraventricular nucleus, d(CH2)5Tyr(Me)2-Orn8-vasotocin (1 microg) reduced almost completely PD-168077-induced penile erection when given into the lateral ventricles[1].
Chemical Properties
Molecular Weight450.49
FormulaC24H26N4O5
Cas No.630117-19-0
SmilesOC(=O)\C=C/C(O)=O.Cc1cccc(c1)C(=O)NCN1CCN(CC1)c1ccccc1C#N
Relative Density.no data available
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: 150 mg/mL (332.97 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.88 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 mM2.2198 mL11.0990 mL22.1981 mL110.9903 mL
5 mM0.4440 mL2.2198 mL4.4396 mL22.1981 mL
10 mM0.2220 mL1.1099 mL2.2198 mL11.0990 mL
20 mM0.1110 mL0.5550 mL1.1099 mL5.5495 mL
50 mM0.0444 mL0.2220 mL0.4440 mL2.2198 mL
100 mM0.0222 mL0.1110 mL0.2220 mL1.1099 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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