Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nemiralisib(GSK-2269557 free base)是一种可口服且具有有效性和特异性的 PI3Kδ 抑制剂,pKi 为 9.9。Nemiralisib 可用于治疗包括慢性阻塞性肺疾病在内的呼吸系统疾病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,190 | 现货 | ||
25 mg | ¥ 2,380 | 现货 | ||
50 mg | ¥ 3,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 818 | 现货 |
产品描述 | Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease. |
靶点活性 | PI3Kγ:5.2 (pic50), PI3Kα:5.3 (pic50), PI3Kβ:5.8 (pic50), PI3Kδ:9.9 (pki) |
体外活性 | Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) (pIC50: 9.7). Nemiralisib is highly selective for PI3Kδ. It has >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50: 5.3), PI3Kβ (pIC50: 5.8), and PI3Kγ (pIC50: 5.2).[1] |
体内活性 | Nemiralisib is active in a disease-relevant brown Norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation. Pharmacokinetic data from Sprague Dawley male rats are obtained to assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route).[1] |
别名 | GSK2269557 (free base), GSK2269557 |
分子量 | 440.54 |
分子式 | C26H28N6O |
CAS No. | 1254036-71-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 29 mg/mL (65.83 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2699 mL | 11.3497 mL | 22.6994 mL | 56.7485 mL |
5 mM | 0.454 mL | 2.2699 mL | 4.5399 mL | 11.3497 mL | |
10 mM | 0.227 mL | 1.135 mL | 2.2699 mL | 5.6749 mL | |
20 mM | 0.1135 mL | 0.5675 mL | 1.135 mL | 2.8374 mL | |
50 mM | 0.0454 mL | 0.227 mL | 0.454 mL | 1.135 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。
Nemiralisib 1254036-71-9 PI3K/Akt/mTOR signaling PI3K GSK 2269557 GSK2269557 (free base) GSK2269557 GSK-2269557 Inhibitor inhibitor inhibit