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GSK180736A

Name: GSK180736A
Brand: TargetMol
SKU: T3513
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3513Cas No. 817194-38-0

Alias GSK180736

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

GSK180736A

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Purity: 99.51%

Catalog No. T3513Alias GSK180736Cas No. 817194-38-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$35	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$67	In Stock	In Stock
10 mg	$90	In Stock	In Stock
25 mg	$173	In Stock	In Stock
50 mg	$323	In Stock	In Stock
100 mg	$598	In Stock	In Stock
500 mg	$1,290	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$59	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.51%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
Targets&IC50	ROCK1:100 nM, GRK2:0.77 μM
In vitro	GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5[2]. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM)[3].
Cell Research	Cardiac myocytes are isolated from LV free wall and septum of C57/Bl6 mice. Cells are treated with isoproterenol (0.5 μM) for 2 min for the recording of contraction, with pretreatment of either PBS as vehicle or paroxetine (10 μM), 215022 (0.1, 0.5, 1, 10 μM), 215023 (0.1, 0.5, 1, 10 μM), 224064 (0.1, 0.5, 1, 10 μM), and GSK180736A ( 0.5, 1 μM), for 10 min[1].
Synonyms	GSK180736

Chemical Properties

Molecular Weight	365.36
Formula	C₁₉H₁₆FN₅O₂
Cas No.	817194-38-0
Smiles	CC1=C(C(NC(=O)N1)c1ccc(F)cc1)C(=O)Nc1ccc2[nH]ncc2c1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 100 mg/mL (273.7 mM), Sonication is recommended.

Ethanol: 3 mg/mL (8.21 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.47 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7370 mL	13.6851 mL	27.3703 mL	136.8513 mL
5 mM	0.5474 mL	2.7370 mL	5.4741 mL	27.3703 mL

DMSO

	1mg	5mg	10mg	50mg
10 mM	0.2737 mL	1.3685 mL	2.7370 mL	13.6851 mL
20 mM	0.1369 mL	0.6843 mL	1.3685 mL	6.8426 mL
50 mM	0.0547 mL	0.2737 mL	0.5474 mL	2.7370 mL
100 mM	0.0274 mL	0.1369 mL	0.2737 mL	1.3685 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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