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GSK269962A
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:850664-21-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
GSK 269962
GSK269962B
GSK269962A HCl
产品介绍
GSK269962A 是一种有效的ROCK抑制剂,具有抗炎和血管舒张作用。它作用于重组人ROCK1和ROCK2,IC50分别为 1.6 和 4 nM。

产品描述

GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

体外活性

GSK269962A completely abolished the actin stress fiber formation induced by angiotensin II in human smooth muscles. Such suppressive effect on actin fiber formation was observed beginning at around 1 μM GSK269962A. GSK269962A induced vasorelaxation in preconstricted rat aorta(tissue baths) with an IC50 of 35 nM. the relaxation induced by GSK269962A is reversible. GSK269962A suppressed IL-6 mRNA transcription and reduced LPS-induced IL-6 and TNF-α protein production in macrophages

体内活性

Oral administration of GSK269962A produced a profound dose-dependent reduction of systemic blood pressure in spontaneously hypertensive rats. The reduction of blood pressure was acute and substantial. The maximal effect on blood pressure was observed approximately 2 h after oral gavages. The reduction of blood pressure was accompanied by an acute, dose-dependent increase in heart rate, presumably due to the activation of baroreflex mechanism. ROCK inhibition with the use of GSK 269962 in the 10 mg/kg dose, in turn, triggered an increase in VV(voided volume), PVR(post-void residual), VT(volume threshold), VE(voiding efficiency), ICI(intercontraction interval), BC(bladder compliance), and VTNVC(volume threshold to elicit NVC).

激酶实验

The enzyme activity and kinetics of the purified ROCK1(3-543) are determined using scintillation proximity assay. In this assay, purified ROCK1 is incubated with peptide substrate (Biotin-Ahx-AKRRLSSLRA-CONH2), and 33ATP and the subsequent incorporation of 33P into the peptide is quantified by streptavidin bead capture. For IC50 determination, test compounds are dissolved at 10 mM in 100% DMSO, with subsequent serial dilution in 100% DMSO. Compounds are typically assayed over an 11-point dilution range with a concentration in the assay of 10 μM to 0.2 nM in 3-fold dilutions. For dose-response curves, data are normalized and expressed as percentage inhibition using the formula 100×[(U-C1)/(C2-C1)], where U is the unknown value, C1 is the average of the high signal (0%) control wells, and C2 is the average of the low signal (100%) control wells. Curve fitting is performed The results for each compound are recorded as pIC50 values[1].

细胞实验

Human primary smooth muscle cells were serum-starved(cells were grown on coverslips, and at approximately 50% confluence, they were serum-starved overnight) and stimulated with AngII (100 nM) for 2 h. ROCK inhibitors (3 μM for SB-772077-B or GSK269962A) were added 30 min before AngII stimulation, and cells were fixed and stained with rhodamine phalloidin. Confocal images of actin stain were obtained.(Only for Reference)

Cas No.

850664-21-0

分子式

C29H30N8O5

分子量

570.61

别名

GSK 269962;GSK269962B;GSK269962A HCl

储存和溶解度

Ethanol:6 mg/mL (9.88 mM)
H2O:<1 mgml
DMSO:57.1 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years