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Cat. No.: HY-120718

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CCG 224061

CCG 224061 is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with a IC₅₀ of 0.066 μM. CCG 224061 inhibits GRK activity in cardiomyocytes. CCG 224061 is applicable to research related to heart disease, heart failure, myocardial hypertrophy and hypertension.

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CAS No.: 2055990-82-2
Formule: C₁₉H₂₀FN₃O
Masse moléculaire:325.39

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Please store the product under the recommended conditions in the Certificate of Analysis.

CCG 224061 Chemical Structure

CAS No.: 2055990-82-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

CCG 224061 is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with a IC₅₀ of 0.066 μM. CCG 224061 inhibits GRK activity in cardiomyocytes^[1]. CCG 224061 is applicable to research related to heart disease, heart failure, myocardial hypertrophy and hypertension^[1]^[2].

IC₅₀ & Target^[1]

GRK2

0.066 μM (IC₅₀)

In Vitro

CCG 224061 (E18) potently and selectively inhibits GRK2 with an IC₅₀ of 0.07 μM, while it shows weak inhibitory effects on GRK5 (IC₅₀ 12.8 μM) and GRK1 (IC₅₀ 65.7 μM)^[1].
CCG 224061 (5 min) potently inhibits GRK2 (IC₅₀ = 0.066 μM) and exhibits activity against GRK1 (IC₅₀ = 6.4 μM), GRK5 (IC₅₀ = 1.3 μM), PKA (IC₅₀ = 3.1 μM) and ROCK1 (100% inhibition at 10 μM) in in vitro purified kinase assays^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	AUC_0-∞
Mice^[2]	10 mg/kg	i.p.	731 ng·h/mL

Chemical Information

CAS No. 2055990-82-2
Masse moléculaire 325.39
Formule C₁₉H₂₀FN₃O
SMILES

C(OC=1C=C2C(=CC1)NN=C2)[C@H]3[C@@H](CCNC3)C4=CC=C(F)C=C4
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Scott D. Larsen, et al. G protein-coupled receptor kinase inhibitors and methods for use of the same. WO2016210403A1. 2017-12-26.

[2]. Bouley R, et al. Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors. Mol Pharmacol. 2017;92(6):707-717. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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