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CAS No.: 1700693-08-8

JH-II-127 Catalog No. CSN17129

Synonyms: JH-II-127

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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 LRRK2 (G2019S)

IC50:2.2nM LRRK2 (A2016T)

IC50:47.7nM LRRK2

IC50:6.6nM
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.

动物研究

剂量

Mice: 10 mg/kg - 50 mg/kg^[1] (p.o.); 2 mg/kg^[1] (i.v.)

给药途径

p.o., i.v.

动物药代数据

Animal	Mice^[1]
Dose	2 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.
AUC_inf	535.57 h·ng/ml (i.v.) 3867.07 h·ng/ml (p.o.)
T_1/2	0.66 h (i.v.)
T_max	1 h (i.v. or p.o.)
C₀/C_max	1604.47 ng/ml (i.v.) 802.72 ng/ml (p.o.)
CL	62.24 ml/min/kg (i.v.)
AUC_last	532.67 h·ng/ml (i.v.) 3094.58 h·ng/ml (p.o.)
Vss	1.73 L/kg (i.v.)

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3989 mL
- 11.9944 mL
- 23.9888 mL
- 5 mM
- 0.4798 mL
- 2.3989 mL
- 4.7978 mL
- 10 mM
- 0.2399 mL
- 1.1994 mL
- 2.3989 mL

技术信息

CAS号

1700693-08-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21ClN6O3

运输

蓝冰

分子量

416.86

别名

JH-II-127

溶解度

DMSO	30.0 mg/mL (72.0 mM)

动物实验配方

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靶点	Description	IC50
LRRK2 (G2019S)		IC50:2.2nM
LRRK2 (A2016T)		IC50:47.7nM
LRRK2		IC50:6.6nM

JH-II-127 Catalog No. CSN17129

靶点选择性

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