HG-10-102-01,1351758-81-0

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HG-10-102-01

CAS No. : 1351758-81-0

MCE 国际站：HG-10-102-01

产品活性：HG-10-102-01 是一种高效、选择性、可透过血脑屏障的 LRRK2 抑制剂，其对于野生型 LRRK2 和 LRRK2[G2019S]， IC₅₀ 值分别为 20.3 和 3.2 nM。HG-10-102-01也能抑制 MNK2 和 MLK1，其 IC₅₀ 值分别为 0.6 和 2.1 μM。HG-10-102-01 可用于帕金森病 (PD) 的研究。

研究领域：Autophagy  |  MAPK/ERK Pathway

作用靶点：LRRK2  |  MNK

In Vitro: HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant.

In Vivo: HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice.
HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure.

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