CZC-25146,1191911-26-8

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CZC-25146

CAS No. : 1191911-26-8

MCE 国际站：CZC-25146

产品活性：CZC-25146 是一种有效且具有口服活性的 LRRK2 抑制剂，对野生型 LRRK2 和突变型 LRRK2 G2019S 的 IC₅₀ 分别为 4.76 nM 和 6.87 nM。也抑制激酶 PLK4、GAK、TNK1、CAMKK2 和 PIP4K2C。CZC-25146 能在体外抑制突变 LRRK2 诱导的神经元损伤。CZC-25146 在小鼠体内表现出相对较好的药代动力学特性。CZC-25146 还能增加正常的 α-1 抗胰蛋白酶 (AAT) 的分泌，减少炎症细胞因子。CZC-25146 可用于帕金森病和肝病的研究。

研究领域：Autophagy

作用靶点：LRRK2

In Vitro: CZC-25146 (0.01-5 μM; 7 days) does not cause cytotoxicity in human cortical neurons, nor blocking neuronal development.
CZC-25146 (0.01-5 μM; 2 days) potently attenuates G2019S LRRK2-mediated toxicity in primary rodent neurons in a concentration-dependent manner with an EC₅₀ of ~100 nM.
CZC-25146 (0.06-1000 nM) rescues LRRK2 G2019S-induced neurite defects in primary human neurons in a dose-dependent manner.
CZC-25146 (14.3 and 28.6 μM; 48 h) markedly reduces The mutant AAT encoded by the Z allele (ATZ) polymer load and restores AAT secretion in iPSC-Hepatocyte, without compromising cell viability.

In Vivo: CZC-25146 (250 mg/kg; p.o.; 14 days) reduces the ATZ polymer levels in over expressing human polymeric ATZ mice.
CZC-25146 (1 mg/kg for i.v.; 5 mg/kg for p.o.; single dosage) exhibits relatively good pharmacokinetic properties and an extensive distribution throughout animal body following intravenous injection into mice.

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