LP-922761 hydrate 是一种有效的，选择性的，具有口服活性的 AAK1 抑制剂，在酶和细胞分析中 IC50 分别为 4.8 nM 和 7.6 nM。LP-922761 hydrate 还抑制 BMP-2 诱导蛋白激酶 (BIKE)，IC50 为 24 nM。LP-922761 hydrate 对细胞 GAK，阿片类药物，肾上腺素 α2 或 GABAa 受体无明显活性。
| 生物活性 |
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors. |
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| IC50&Target |
IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE)) |
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| 体内研究 |
In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： ≥98%
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