Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IHMT-PI3Kδ-372 S-isomer 是一种有效的选择性 PI3Kδ 抑制剂,IC50 为 14 nM。IHMT-PI3Kδ-372 S-isomer 对 PI3Kδ 的选择性高于其他 I 类 PI3K (56-83 倍) 和其他蛋白激酶。IHMT-PI3Kδ-372 S-isomer 可用于慢性阻塞性肺疾病 (COPD )的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,290 | 现货 | ||
2 mg | ¥ 1,930 | 现货 | ||
5 mg | ¥ 2,990 | 现货 | ||
10 mg | ¥ 4,390 | 现货 | ||
25 mg | ¥ 6,910 | 现货 | ||
50 mg | ¥ 9,480 | 现货 | ||
100 mg | ¥ 12,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,490 | 现货 |
产品描述 | IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research. |
体外活性 | IHMT-PI3Kδ-372 (S)-18 (0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC50 value of 67 nM. IHMT-PI3Kδ-372 (S)-18 shows moderate inhibition of CYP2C9 (IC50 of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC50s > 10 μM)[1]. |
体内活性 | IHMT-PI3Kδ-372 (S)-18; 1-5 mg/kg; inhalation; daily; for 28 days) improves lung function and reduced the inflammatory patterns characteristic of COPD. The lung function parameters such as forced expiratory volume in the first second (FEV1), forced vital capacity (FVC), and peak expiratory flow (PEF) are improved dose-dependently. The abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes are also reduced. IHMT-PI3Kδ-372 (S)-18 decreases the inflammatory cell infiltration in a dose-dependent manner. In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (S)-18 displays a half-life of 2.3 h, low exposure of 66 ng/mL, and high clearance of 348.5 mL/min/kg in plasma but high exposure of 5599 ng/g (6 h after inhalation) in lung tissue. IHMT-PI3Kδ-372 (S)-18 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes[1]. |
分子量 | 503.5 |
分子式 | C26H23F2N7O2 |
CAS No. | 2429889-61-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (99.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9861 mL | 9.9305 mL | 19.861 mL | 49.6524 mL |
5 mM | 0.3972 mL | 1.9861 mL | 3.9722 mL | 9.9305 mL | |
10 mM | 0.1986 mL | 0.993 mL | 1.9861 mL | 4.9652 mL | |
20 mM | 0.0993 mL | 0.4965 mL | 0.993 mL | 2.4826 mL | |
50 mM | 0.0397 mL | 0.1986 mL | 0.3972 mL | 0.993 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。
IHMT-PI3Kδ-372 S-isomer 2429889-61-0 PI3K/Akt/mTOR signaling PI3K IHMTPI3Kδ372Sisomer IHMT-PI3Kdelta-372 S-isomer Inhibitor inhibitor inhibit