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。

LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1 ) inhibitor with IC 50 s 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 IC 50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors [1].

In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment [1].

C21H28N6O4

414.98

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years