Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW788388 是一种 ALK5抑制剂(IC50:18 nM)。它也抑制 TGF-β II 型受体和激活素 II 型受体的活性,但对 BMP II 型受体无影响。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 216 | 现货 | ||
5 mg | ¥ 475 | 现货 | ||
10 mg | ¥ 789 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 2,530 | 现货 | ||
100 mg | ¥ 3,770 | 现货 | ||
500 mg | ¥ 8,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 475 | 现货 |
产品描述 | GW788388 is a potent and selective inhibitor of ALK5, also inhibits TGF-(beta) type II receptor and activin type II receptor activities. |
靶点活性 | ALK5:18 nM |
体外活性 | 在嘌呤霉素氨基核甙诱导的肾脏纤维化模型中,GW788388(10 mg/kg)能够诱导胶原A1 mRNA 表达.在患晚期糖尿病肾病鼠中,GW788388通过减少TGF-β 信号,降低纤维反应.在心肌梗塞鼠中,GW788388处理后,能够明显抑制收缩功能,降低心肌细胞肥大 ,且降低激活的Smad2, α-SMA. |
体内活性 | GW788388能够抑制ALK5, ALK4, ALK7 和TGF-β调节的生长。在细胞实验中(IC50=93 nM),GW788388具有抗TGF-β诱导的Smad激活,且抑制靶点基因表达。 |
激酶实验 | ALK5 Fluorescence Polarization Binding Assay: GW788388 binding to ALK5 is tested on purified recombinant GST?ALK5 (residues 198-503). Displacement of rhodamine green fluorescently labeled ATP competitive inhibitor by different concentrations of GW788388 is used to calculate a binding pIC50. GST?ALK5 is added to a buffer containing 62.5 mM N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid (Hepes), pH 7.5, 1 mM dithiothreitol (DTT), 12.5 mM MgCl2, 1.25 mM 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonic acid (CHAPS), and 1 nM rhodamine green-labeled ligand so that the final ALK5 concentration is 10 nM based on active-site titration of the enzyme. The enzyme/ligand reagent (40 μL) is added to 384-well assay plates containing 1 μL of different concentrations of GW788388. The plates are read immediately on a LJL Acquest fluorescence reader with excitation, emission, and dichroic filters of 485, 530, and 505 nm, respectively. The fluorescence polarization for each well is calculated by the Acquest and is then imported into curve-fitting software for construction of concentration?response curves. |
细胞实验 | Cell viability/proliferation assays are done according to the manufactures instructions (CellTiter 96 Aqueous One Solution Cell Proliferation Assay). Viability and proliferation are measured after 72 hours GW788388 treatment in the presence or absence of TGF-β.(Only for Reference) |
别名 | GW 788388 |
分子量 | 425.48 |
分子式 | C25H23N5O2 |
CAS No. | 452342-67-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 42.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3503 mL | 11.7514 mL | 23.5029 mL | 58.7572 mL |
5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | 11.7514 mL | |
10 mM | 0.235 mL | 1.1751 mL | 2.3503 mL | 5.8757 mL | |
20 mM | 0.1175 mL | 0.5876 mL | 1.1751 mL | 2.9379 mL | |
50 mM | 0.047 mL | 0.235 mL | 0.4701 mL | 1.1751 mL | |
100 mM | 0.0235 mL | 0.1175 mL | 0.235 mL | 0.5876 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。
GW788388 452342-67-5 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad inhibit Transforming growth factor beta receptors GW-788388 TGF-β Receptor Inhibitor GW 788388 inhibitor