Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) 是一种选择性的 RGS4 抑制剂,对 RGS4-Gαo 蛋白-蛋白相互作用的 IC50 为 17 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
2 mg | ¥ 1,720 | 现货 | ||
5 mg | ¥ 2,790 | 现货 | ||
10 mg | ¥ 4,150 | 现货 | ||
25 mg | ¥ 6,630 | 现货 | ||
50 mg | ¥ 8,850 | 现货 | ||
100 mg | ¥ 11,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,990 | 现货 |
产品描述 | CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction. |
靶点活性 | RGS16:6 μM, RGS8:79 μM, RGS4:17 nM, RGS19:140 nM, GSK3β:5.4 μM |
体外活性 | CCG 203769 displays dramatic selectivity (8- to >5000-fold) for RGS4 over other RGS proteins with IC50s of 140 nM, 6 μM, and 79 μM for RGS19, RGS16, and RGS8. CCG 203769 inhibits GSK-3β with an IC50 of 5 μM. CCG 203769 enhances Gαq-dependent cellular Ca2+ signaling in an RGS4-dependent manner and inhibits RGS/Gαo binding in an RGS-selective manner. CCG 203769 also blocks the GTPase accelerating protein (GAP) activity of RGS4. CCG 203769 inhibits the effect of GTP hydrolysis stimulated by RGS4 with an IC50<1 μM in single-turnover and steady-state GTPase experiments[1]. |
体内活性 | CCG 203769 (10 mg/kg, i.v.), administered immediately prior to Carbamoylcholine chloride(0.1 mg/kg, i.p.), significantly potentiates the bradycardic effect. CCG 203769 (1-10 mg/kg) reverses the increased hang time caused by raclopride administration in rats. CCG 203769 (0.1-10 mg/kg) reverses the raclopride-induced paw drag in mice[1]. |
别名 | 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, RGS4 inhibitor 11b, Thiadiazolidinone (TDZD) deriv. 6 |
分子量 | 202.27 |
分子式 | C8H14N2O2S |
CAS No. | 410074-60-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (247.2 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 | 4.9439 mL | 24.7194 mL | 49.4389 mL | 123.5972 mL |
5 mM | 0.9888 mL | 4.9439 mL | 9.8878 mL | 24.7194 mL | |
10 mM | 0.4944 mL | 2.4719 mL | 4.9439 mL | 12.3597 mL | |
20 mM | 0.2472 mL | 1.236 mL | 2.4719 mL | 6.1799 mL | |
50 mM | 0.0989 mL | 0.4944 mL | 0.9888 mL | 2.4719 mL | |
100 mM | 0.0494 mL | 0.2472 mL | 0.4944 mL | 1.236 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。
CCG 203769 410074-60-1 GPCR/G Protein Neuroscience PI3K/Akt/mTOR signaling Stem Cells Dopamine Receptor GSK-3 GTPase CCG203769 CCG-203769 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione RGS4 inhibitor 11b Thiadiazolidinone (TDZD) deriv. 6 Inhibitor inhibitor inhibit