GRK5-IN-5
GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 3061801-11-1
- 화학식: C30H27FN4O5
- 분자량:542.56
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[1]|
GRK5 0.03 μM (IC50) |
GRK6 0.036 μM (IC50) |
GRK2 2.2 μM (IC50) |
Chemical Information
-
CAS No. 3061801-11-1
-
분자량 542.56
-
화학식 C30H27FN4O5
-
SMILES
O=C(C1=CC2=C(NC(/C2=C\C3=C(C)C(NC([C@@H](O)C4=CC=CO4)=O)=C(C)N3)=O)C=C1)N[C@H](C)C5=CC=C(F)C=C5
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Cardiac Morphometry
Cardiac morphometry is based on quantitative histological and stereological assessment of myocardial structure, including cardiomyocyte size, number, and extracellular matrix composition, to evaluate cardiac growth and remodeling under physiological or pathological conditions. Design-based stereology is considered a reference framework for obtaining unbiased estimates of structural parameters such as cardiomyocyte number, volume, and tissue architecture, enabling quantitative comparison across experimental groups. Histological image-based morphometry further enables measurement of cardiomyocyte cross-sectional area and collagen deposition using microscopy combined with image analysis software, allowing assessment of hypertrophy and fibrosis in cardiac remodeling models. These morphometric readouts reflect underlying biological processes such as cardiomyocyte hypertrophy, loss, or structural reorganization during disease progression or experimental stress.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)