CZC-54252 hydrochloride 是 LRRK2 的特异性抑制剂,对野生型和 G2019S LRRK2 的 IC50 分别为 1.85 nM 和 1.28 nM。 CZC-54252 hydrochloride 具有神经保护活性,可减轻 G2019S LRRK2 诱导的人类神经元损伤,EC50 为 1 nM。
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描述
CZC-54252 hydrochloride is a selective inhibitor of LRRK2 with IC50s of 1.85 nM and 1.28 nM for wild-type and G2019S LRRK2. CZC-54252 hydrochloride has a neuroprotective activity and attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of 1 nM.
体外活性
CZC-54252 hydrochloride(1.6 nM) fully reverses G2019S LRRK2-induced human neuronal injury to wild-type levels. CZC-54252 hydrochloride inhibits the recombinant human wild-type LRRK2 with an IC50 ranging from 1 to 5 nM. CZC-54252 hydrochloride inhibits the G2019S mutant with an IC50 ranging from 2 to 7 nM in a TF-FRET assay[2].
Cas No.
1784253-05-9
分子式
C22H26Cl2N6O4S
分子量
541.45
储存和溶解度
DMSO:30 mg/mL (55.41 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years