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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 457 | 现货 | |
5 mg | ¥ 1,120 | 现货 | |
10 mg | ¥ 1,780 | 现货 | |
25 mg | ¥ 2,950 | 现货 | |
50 mg | ¥ 4,140 | 现货 | |
100 mg | ¥ 5,690 | 现货 | |
500 mg | 询价 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,250 | 现货 |
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. |
靶点活性 | PI3Kδ:14 nM (IC50), CYP2C9:2.7 μM (IC50) |
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]. |
别名 | IHMT-PI3Kδ-372 |
分子量 | 503.5 |
分子式 | C26H23F2N7O2 |
CAS No. | 2429889-62-1 |
Smiles | CC[C@H](c1nc2cccc(F)c2c(=O)n1C1CC1)n1nc(-c2ccc(OC)c(F)c2)c2c(N)ncnc12 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 37.8 mg/mL (75.1 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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