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GSK180736A

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Purity:98.44%

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COA HPLC LCMS HNMR

GSK180736A

Catalog No. T3513Cas No. 817194-38-0

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).

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

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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).
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].
Alias	GSK180736

Chemical Properties

Molecular Weight	365.36
Formula	C19H16FN5O2
Cas No.	817194-38-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

DMSO: 60 mg/mL (164.22 mM)

Ethanol: 3 mg/mL (8.21 mM)

Solution Preparation Table

DMSO/Ethanol

	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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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