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PF-5190457

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Catalog No. T16508Cas No. 1334782-79-4
Alias PF-05190457

PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36).

PF-5190457

PF-5190457

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Purity: 99.34%
Catalog No. T16508Alias PF-05190457Cas No. 1334782-79-4
PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
2 mg$44In StockIn Stock
5 mg$72In StockIn Stock
10 mg$128In StockIn Stock
25 mg$289In StockIn Stock
50 mgPreferential-In Stock
1 mL x 10 mM (in DMSO)$82In 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:99.34%
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Product Introduction

Bioactivity
Description
PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36).
Targets&IC50
Ghrelin receptor:8.36 (pKi)
In vitro
PF-5190457 demonstrates an optimal balance of ghrelin receptor pharmacology along with off-target selectivity [1].
In vivo
In human whole and dispersed islets, PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion[1].
SynonymsPF-05190457
Chemical Properties
Molecular Weight512.67
FormulaC29H32N6OS
Cas No.1334782-79-4
SmilesCc1cn2cc(CC(=O)N3CCC4(CN(C4)[C@@H]4CCc5cc(ccc45)-c4cc(C)ncn4)CC3)nc2s1
Relative Density.1.41 g/cm3 (Predicted)
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: 7.1 mg/mL (13.85 mM), Sonication is recommended.
Ethanol: 100 mg/mL (195.06 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.75 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/Ethanol
1mg5mg10mg50mg
1 mM1.9506 mL9.7529 mL19.5057 mL97.5286 mL
5 mM0.3901 mL1.9506 mL3.9011 mL19.5057 mL
10 mM0.1951 mL0.9753 mL1.9506 mL9.7529 mL
Ethanol
1mg5mg10mg50mg
20 mM0.0975 mL0.4876 mL0.9753 mL4.8764 mL
50 mM0.0390 mL0.1951 mL0.3901 mL1.9506 mL
100 mM0.0195 mL0.0975 mL0.1951 mL0.9753 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

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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

Keywords

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