Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CMPD101 是膜透性的 GRK2/3高选择性小分子抑制剂,IC50分别为 18 nM 和 5.4 nM。它针对 GRK1、GRK5 ROCK-2 和 PKCα 的选择性较小,IC50值分别为 3.1 μM,2.3 μM,1.4 μM 和 8.1 μM,可研究心衰疾病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 487 | 现货 | ||
5 mg | ¥ 1,310 | 现货 | ||
10 mg | ¥ 2,120 | 现货 | ||
25 mg | ¥ 3,630 | 现货 | ||
50 mg | ¥ 5,250 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,360 | 现货 |
产品描述 | CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. |
靶点活性 | PKCα:8.1 μM, ROCK2:1.4 μM, GRK2:18 nM, GRK3:5.4 nM |
体外活性 | CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, significantly reduces the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line[1]. CMPD101 (3-30 μM; pre-30 minutes) does not influence the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30?μM. This compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375. Which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101and it also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues[2]. |
分子量 | 466.46 |
分子式 | C24H21F3N6O |
CAS No. | 865608-11-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (535.95 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1438 mL | 10.719 mL | 21.4381 mL | 53.5952 mL |
5 mM | 0.4288 mL | 2.1438 mL | 4.2876 mL | 10.719 mL | |
10 mM | 0.2144 mL | 1.0719 mL | 2.1438 mL | 5.3595 mL | |
20 mM | 0.1072 mL | 0.536 mL | 1.0719 mL | 2.6798 mL | |
50 mM | 0.0429 mL | 0.2144 mL | 0.4288 mL | 1.0719 mL | |
100 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.536 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。
CMPD101 865608-11-3 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling GPCR/G Protein Stem Cells PKC GRK ROCK Rho-associated kinase Rho-kinase ROK desensitization Inhibitor inhibit CMPD-101 failure Neuron CMPD 101 Protein kinase C heart Rho-associated protein kinase inhibitor