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IHMT-PI3Kδ-372

CAS No. : 2429889-62-1

MCE 站：IHMT-PI3Kδ-372

产品活性：IHMT-PI3Kδ-372 是一种有效的选择性 PI3Kδ 抑制剂，IC₅₀ 为 14 nM。IHMT-PI3Kδ-372 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 可用于慢性阻塞性肺疾病 (COPD )的研究。

研究领域：PI3K/Akt/mTOR  |  Metabolic Enzyme/Protease

作用靶点：PI3K  |  Cytochrome P450

In Vitro: IHMT-PI3Kδ-372 (Compound (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 (compound (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).

In Vivo: IHMT-PI3Kδ-372 (Compound (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 decreases the inflammatory cell infiltration in a dose-dependent manner.
In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (compound (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 is stable in human, rat, ａnd mouse liver microsomes, while it has moderate stability in monkey ａnd dog liver microsomes.

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