JH-II-127
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货号：A248253
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.
JH-II-127 化学结构
JH-II-127 3D分子结构
规格
价格
会员价
库存
数量
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JH-II-127 纯度/质量文件 产品仅供科研
货号：A248253
标准纯度：
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产品说明书
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JH-II-127 质控信息
GNE-7915
++++
LRRK2, Ki: 1 nM
LRRK2, IC50: 9 nM
99%+
GNE-9605
+++
LRRK2, Ki: 2 nM
LRRK2, IC50: 19 nM
99%+
GSK2578215A
++
LRRK2 (G2019S), IC50: 8.9 nM
LRRK2 (WT), IC50: 10.9 nM
99%+
URMC-099
+
99%+
PF-06447475
+++
99%+
LRRK2-IN-1
++
LRRK2 (G2019S), IC50: 6 nM
LRRK2 (WT), IC50: 13 nM
99%+
GNE0877
++++
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
JH-II-127 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.
JH-II-127 动物研究
Dose
Mice: 10 mg/kg - 50 mg/kg[1] [1]
Administration
p.o., i.v.
Pharmacokinetics
Animal
Mice[1]
Dose
2 mg/kg (i.v.)
Administration
i.v.
AUCinf
535.57 h·ng/ml (i.v.)
T1/2
0.66 h (i.v.)
Tmax
1 h (i.v. or p.o.)
C0 /Cmax
1604.47 ng/ml (i.v.)
CL
62.24 ml/min/kg (i.v.)
AUClast
532.67 h·ng/ml (i.v.)
Vss
1.73 L/kg (i.v.)
JH-II-127 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.
JH-II-127 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
JH-II-127 技术信息
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