JH-II-127

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Chemical Structure| 1700693-08-8 同义名 : -
CAS号 : 1700693-08-8
货号 : A248253
分子式 : C19H21ClN6O3
纯度 : 98%+
分子量 : 416.86
MDL号 : MFCD28975160
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(251.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Among the genes associated with Parkinson’s disease (PD), leucine-rich repeat kinase-2 (LRRK2) is unique, as a missense mutation, G2019S, is frequently found in both familial and sporadic PD cases. JH-II-127 is a brain-penetrant, potent and selective LRRK2 inhibitor with IC50 values of 2.2, 6.6 and 47.7 nM for G2019S-mutant, wild-type and A2016T-mutant LRRK2, respectively, and completely inhibits LRRK2 in mouse brain at 100 mg/kg[2].
作用机制 JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.99mL

2.40mL

1.20mL

23.99mL

4.80mL

2.40mL
参考文献

[1]Hatcher JM, Zhang J, 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.

[2]Hatcher JM, Zhang J, Choi HG, Ito G, Alessi DR, Gray NS. 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):584-9. doi: 10.1021/acsmedchemlett.5b00064. PMID: 26005538; PMCID: PMC4434483.