country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-109562

Copy Link Print Information

CCG258208

(Synonyms: GRKs-IN-1)

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC₅₀=30 nM) while maintaining 230-fold selectivity over GRK5 (IC₅₀=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC₅₀=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 2055990-90-2
화학식: C₂₄H₂₅FN₄O₄
분자량:452.48

보관:

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

Data Sheet (272 KB)

CCG258208 Chemical Structure

CAS No.: 2055990-90-2

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

GRK2

30 nM (IC₅₀)

GRK5

7.1 μM (IC₅₀)

In Vitro

CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes^[1].

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

Cell Viability Assay^[1]

Cell Line:

Mouse cardiomyocytes
Concentration:

0, 0.1, 0.5, and 1 μM
Incubation Time:

10 min
Result:

Showed a significant increase in contractility at a concentration of only 0.1 µM.

In Vivo

CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo^[1].

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

Animal Model:

CD-1 mice^[1]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; 10 mg/kg; once
Result:

Showed total plasma drug levels after single IP administration that exceed the GRK2 IC₅₀ for seven hours.

Chemical Information

CAS No. 2055990-90-2
분자량 452.48
화학식 C₂₄H₂₅FN₄O₄
SMILES

FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1
Synonyms

GRKs-IN-1
선적

Room temperature in continental US; may vary elsewhere.
보관

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

Publications (1)

All

Sort by:

Journal Impact Factor

Commun Biol

Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]

2026 Jan 16;9(1):287. PMID: 41545717

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

CCG258208

1 Cited Publications

100 mg 견적 받기

Subscribe to the

MedChemExpress

Newsletter

MOQ

Minimum order quantity

100 mg

견적 받기 해외재고보유

Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

CCG258208

Publications Citing Use of MedChemExpress (MCE) CCG258208

Biological Activity

Chemical Information

Publications (1)

순도&문서

References

Calculators

Help & FAQs

CCG258208 Related Classifications

HY-109562 Related Classifications