Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK269962A (GSK269962A HCl) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 245 | 现货 | ||
2 mg | ¥ 346 | 现货 | ||
5 mg | ¥ 617 | 现货 | ||
10 mg | ¥ 1,150 | 现货 | ||
25 mg | ¥ 1,950 | 现货 | ||
50 mg | ¥ 2,890 | 现货 | ||
100 mg | ¥ 4,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 775 | 现货 |
产品描述 | GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. |
靶点活性 | ROCK1:1.6 nM, ROCK2:4 nM |
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) |
别名 | GSK269962B, GSK 269962, GSK269962A HCl |
分子量 | 570.6 |
分子式 | C29H30N8O5 |
CAS No. | 850664-21-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 6 mg/mL (9.88 mM)
DMSO: 57.1 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.7525 mL | 8.7627 mL | 17.5254 mL | 43.8135 mL |
5 mM | 0.3505 mL | 1.7525 mL | 3.5051 mL | 8.7627 mL | |
DMSO | 10 mM | 0.1753 mL | 0.8763 mL | 1.7525 mL | 4.3814 mL |
20 mM | 0.0876 mL | 0.4381 mL | 0.8763 mL | 2.1907 mL | |
50 mM | 0.0351 mL | 0.1753 mL | 0.3505 mL | 0.8763 mL | |
100 mM | 0.0175 mL | 0.0876 mL | 0.1753 mL | 0.4381 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK269962A 850664-21-0 Cell Cycle/Checkpoint Cytoskeletal Signaling MAPK PI3K/Akt/mTOR signaling Stem Cells ROCK S6 Kinase anti-inflammatory pressure blood antihypertensive Rho-associated protein kinase GSK269962 Inhibitor GSK269962B Rho-associated kinase GSK-269962 ROK ROCK2 inhibit GSK-269962A GSK 269962 vasodilatory Rho-kinase GSK269962A HCl ROCK1 cardiovascular inhibitor