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CCG258208 hydrochloride

Name: CCG258208 hydrochloride
Brand: TargetMol
SKU: T35875
Price: 117 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T35875

Alias GRK2-IN-1 hydrochloride

CCG258208 hydrochloride (compound 14as hydrochloride) is a highly potent and selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 30 nM. It exhibits >200-fold selectivity for GRK2 over GRK5 (IC50 = 7.1μM). In cardiovascular research, CCG258208 effectively enhances the contractility of beta-AR-stimulated cardiomyocytes by inhibiting GRK2 activity. Additionally, the compound demonstrates excellent in vivo stability, making it a valuable tool for studying GRK2-related conditions such as heart failure.

CCG258208 hydrochloride

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Catalog No. T35875Alias GRK2-IN-1 hydrochloride

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$117	-	In Stock
5 mg	Preferential	-	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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Appearance:Liquid

Color:Transparent

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Product Introduction

Bioactivity

Description	CCG258208 hydrochloride (compound 14as hydrochloride) is a highly potent and selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 30 nM. It exhibits >200-fold selectivity for GRK2 over GRK5 (IC50 = 7.1μM). In cardiovascular research, CCG258208 effectively enhances the contractility of beta-AR-stimulated cardiomyocytes by inhibiting GRK2 activity. Additionally, the compound demonstrates excellent in vivo stability, making it a valuable tool for studying GRK2-related conditions such as heart failure.
Targets&IC50	GRK2:30 nM, GRK5:7.1 uM
In vitro	CCG258208 hydrochloride potently inhibits GRK2 (IC50=30 nM) with minimal activity against GRK5. In mouse cardiomyocytes, it (0.1-1 μM, 10 min) significantly enhances β-AR-stimulated contractility, with effects observed at concentrations as low as 0.1 μM [1].
In vivo	In pharmacological studies using CD-1 mice, a single intraperitoneal (IP) injection of CCG258208 hydrochloride (10 mg/kg) demonstrates favorable pharmacokinetic properties. The treatment maintains total plasma drug levels that exceed the GRK2 IC50 for approximately seven hours [1].
Synonyms	GRK2-IN-1 hydrochloride

Chemical Properties

Molecular Weight	488.94
Formula	C₂₄H₂₆ClFN₄O₄
Smiles	FC(C=C1)=C(C(NCC2=CC=NN2)=O)C=C1[C@H]3[C@H](COC4=CC5=C(OCO5)C=C4)CNCC3.Cl

Storage & Solubility Information

Storage

keep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 40.00 mg/mL (81.81 mM), Sonication is recommended.

DMSO: 200.00 mg/mL (409.05 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.40 mg/mL (4.91 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

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0452 mL	10.2262 mL	20.4524 mL	102.2620 mL
5 mM	0.4090 mL	2.0452 mL	4.0905 mL	20.4524 mL
10 mM	0.2045 mL	1.0226 mL	2.0452 mL	10.2262 mL
20 mM	0.1023 mL	0.5113 mL	1.0226 mL	5.1131 mL
50 mM	0.0409 mL	0.2045 mL	0.4090 mL	2.0452 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0205 mL	0.1023 mL	0.2045 mL	1.0226 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