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GSK269962A

GSK269962A

产品编号 T3518   CAS 850664-21-0
别名: GSK269962B, GSK 269962, GSK269962A HCl

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。

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GSK269962A Chemical Structure
GSK269962A, CAS 850664-21-0
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
其他形式的 GSK269962A:
产品目录号及名称: GSK269962A (T3518)
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纯度: 99.14%
纯度: 98.63%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 6 mg/mL (9.88 mM)

DMSO: 57.1 mg/mL(100 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Doe C, et al. J Pharmacol Exp Ther. 2007, 320(1):89-98. 2. Andrzej Wróbel, et al. Neurourology and Urodynamics. 2016. 3. Xu Q, Fu Q, Li Z, et al. Procyanidin C1 is a natural agent with senolytic activity against aging and age-related diseases[J]. bioRxiv. 2021 4. Mondal T, Shivange G N, Tihagam R G T, et al. Unexpected PD‐L1 immune evasion mechanism in TNBC, ovarian, and other solid tumors by DR5 agonist antibodies. EMBO Molecular Medicine. 2021: e12716.

文献引用

1. Xu Q, Fu Q, Li Z, et al. Procyanidin C1 is a natural agent with senolytic activity against aging and age-related diseases. EMBO Molecular Medicine. (2021)13:e12716 2. Mondal T, Shivange G N, Tihagam R G T, et al. Unexpected PD‐L1 immune evasion mechanism in TNBC, ovarian, and other solid tumors by DR5 agonist antibodies. EMBO Molecular Medicine. 2021 Mar 5;13(3):e12716. doi: 10.15252/emmm.202012716. Epub 2021 Feb 15.
CYC-116 Eudesmin LJI308 PF-4708671 FMK LY-2584702 hydrochloride GSK1838705A CCT128930

相关化合物库

该产品包含在如下化合物库中:
TGF-β/Smad靶点化合物库 抗卵巢癌化合物库 抗抑郁症化合物库 抗胰腺癌化合物库 糖酵解化合物库 抗结直肠癌化合物库 抗癌化合物库 干细胞分化化合物库 抑制剂库 抗癌细胞代谢库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

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