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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.

For research use only. We do not sell to patients.

CAS No.: 2055990-82-2
Formula: C₁₉H₂₀FN₃O
Molecular Weight:325.39

Storage:

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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
Molecular Weight 325.39
Formula C₁₉H₂₀FN₃O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

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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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