438194
LRRK2 Inhibitor II, CZC-25146
The LRRK2 Inhibitor II, CZC-25146 controls the biological activity of LRRK2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
LRRK2 Inhibitor II, CZC-25146, N-(2-(5-Fluoro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl, N-(2-(2-(2-Methoxy-4-morpholinophenylamino)-5-fluoropyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
gray to off-white
溶解性
water: 1 mg/mL
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
FC1=C(N=C(NC2=CC=C(N3CCOCC3)C=C2OC)N=C1)NC4=CC=CC=C4NS(=O)(C)=O.[xHCl]
一般描述
An orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50 = 4.76 and 6.87 nM for hr-wt-LRRK2 and G2019S-LRRK2 mutant, respectively) with selectivity over PLK4, GAK, TNK1, CAMKK2, and PIP4K2C (IC50<300 nM) in a 185-kinase panel. Does neither exert cytotoxicity nor block neuronal development of human or rat cortical neurons at 1 µM. Shown to prevent GS-LRRK2-induced neuronal injury (EC50 ~4 nM) and G2019S- or R1441C-LRRK2-mediated neuronal death in both rat and human cortical neurons (EC50 ~ 100 nM). Even though exhibits favorable pharmacokinetic profile and metabolic stability, and yet suffers from limited blood brain barrier penetration (~4%).
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Ramsden, N., et al. 2011. ACS Chem. Biol.6, 1021.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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