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JH-II-127
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
JH-II-127图片
CAS NO:1700693-08-8
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
JH-II-127 是一种具有口服活性、高效、选择性和脑可渗透的 LRRK2 抑制剂，对野生型 LRRK2 和 LRRK2-G2019S 和突变型 LRRK2-A2016T 的 IC50 分别为 6、2 和 48 nM。
Cas No.1700693-08-8
Canonical SMILESO=C(C1=CC=C(NC2=NC3=NC=C(Cl)C3=C(NC)N2)C(OC)=C1)N4CCOCC4
分子式C19H21ClN6O3
分子量416.86
溶解度DMSO : ≥ 30 mg/mL (71.97 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 uM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.

References:
[1]. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-589.