化合物IHMT-PI3Kδ-372 T35530

Product Introduction
Bioactivity


英文名: IHMT-PI3Kδ-372

描述: IHMT-PI3Kδ-372 是一种选择性的 PI3Kδ 抑制剂，IC50 为 14 nM，可用于慢性阻塞性肺病的研究。

体外活性: In Raji cells, IHMT-PI3Kδ-372 (0.03-3 μM) inhibits PI3Kδ-mediated AKT T308 phosphorylation (EC50 = 67 nM).IHMT-PI3Kδ-372 moderately inhibits CYP2C9 (IC50 = 2.7 μM) and no apparently inhibits CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC50s > 10 μM)[1].

体内活性: IHMT-PI3Kδ-372 (1-5 mg/kg; inhalation) improves lung function and reduced the inflammatory patterns characteristic of COPD with better forced expiratory volume in FEV1, FVC, and PEF. IHMT-PI3Kδ-372 dose-dependently decreases the inflammatory cell and reduces the abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes. In rats, IHMT-PI3Kδ-372 (5 mg/kg; inhalation) 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 and high exposure of 5599 ng/g (6 h after inhalation) in lung tissue[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 37.8 mg/mL (75.1 mM)


关键字: IHMT-PI3Kdelta-372 | IHMTPI3Kδ372 | IHMT-PI-3Kδ-372 | IHMT PI3Kδ 372

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途