Shanghai Nianxing Industrial Co., Ltd
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Product Name: LRRK2-IN-7
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2307277-93-4

2307277-93-4 structure

2307277-93-4 structure

Name: LRRK2-IN-7
Chemical Name: LRRK2-IN-7
CAS Number: 2307277-93-4
Molecular Formula: C₂₄H₂₆N₆O
Molecular Weight: 414.50
Catalog: Signaling Pathways Autophagy LRRK2
Create Date: 2023-01-31 16:06:01
Modify Date: 2024-04-10 19:11:09
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1].

Name	LRRK2-IN-7

Description	LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1].
Related Catalog	Signaling Pathways >> Autophagy >> LRRK2 Research Areas >> Neurological Disease
Target	IC50: 0.9 nM (LRRK2 Kinase)[1]
In Vitro	LRRK2-IN-7 (compound 25) 既是小鼠乳腺癌抗性蛋白 (BCRP) 底物（小鼠/人 BCRP）也是一种有效的人 BCRP 抑制剂（BCRP IC50 = 0.12 μM）[1] .
In Vivo	在一项为期 7 天的大鼠剂量限制毒性研究中，LRRK2-IN-7 (compound 25) 的耐受性高达 100 mg/kg，每天一次（AUCtot = 330 μM·h）[1]。在大鼠急性（2 小时）PK/PD 研究中，LRRK2-IN-7 (compound 25) 显示大鼠脑纹状体中 LRRK2 pS935 剂量依赖性降低，EC50 = 0.18 nM[1]。
References	[1]. David A Candito, et al. Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1 H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease. J Med Chem. 2022 Dec 22;65(24):16801-16817.

Molecular Formula	C₂₄H₂₆N₆O
Molecular Weight	414.50

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