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。
产品描述
IHMT-PI3Kδ-372 is a selective inhibitor of PI3Kδ with an IC50 of 14 nM and can be used in studies about chronic obstructive pulmonary disease.
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].
Cas No.
2429889-62-1
分子式
C26H23F2N7O2
分子量
503.5
别名
IHMT-PI3Kδ-372
储存和溶解度
DMSO:37.8mg/mL (75.1mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years