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Merck
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SML2296

Sigma-Aldrich

GSK180736A

≥98% (HPLC)

同義詞:

4-(4-Fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide, GSK 180736A

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About This Item

經驗公式(希爾表示法):
C19H16FN5O2
CAS號碼:
分子量::
365.36
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

O=C(NC1=CC=C(NN=C2)C2=C1)C3=C(C)NC(NC3C4=CC=C(F)C=C4)=O

生化/生理作用

GSK180736A is a potent and selective dual inhibitor of a ROCK1 (Rho-associated, coiled-coil-containing protein kinase) and GRK2 (G protein-coupled receptor kinase 2). GSK180736A binds to the GRK2 active site. GSK180736A produces a significant cardiomyocytes contraction at 1 μM.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Kristoff T Homan et al.
ACS chemical biology, 10(1), 310-319 (2014-09-23)
Selective inhibitors of individual subfamilies of G protein-coupled receptor kinases (GRKs) would serve as useful chemical probes as well as leads for therapeutic applications ranging from heart failure to Parkinson's disease. To identify such inhibitors, differential scanning fluorimetry was used
Renee Bouley et al.
Molecular pharmacology, 92(6), 707-717 (2017-10-27)
G protein-coupled receptor kinases (GRKs) phosphorylate activated receptors to promote arrestin binding, decoupling from heterotrimeric G proteins, and internalization. GRK2 and GRK5 are overexpressed in the failing heart and thus have become therapeutic targets. Previously, we discovered two classes of
Clark A Sehon et al.
Journal of medicinal chemistry, 51(21), 6631-6634 (2008-10-10)
Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of this enzyme in many aspects of cardiovascular function. Here we report a series of ROCK1 inhibitors which

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