|N-(2-((5-氯-2-((2-甲氧基-4-吗啉苯基)氨基)嘧啶-4-基)氨基)苯基)甲磺酸|CsnPharm

CAS No.: 1191911-27-9

CZC-54252 Catalog No. CSN16309

Synonyms: CZC-54252

CZC-54252 is a potent LRRK2 inhibitor with IC50 values of 1.28 nM and 1.85 nM for wild-type and G2019S mutant LRRK2, respecitively, possessing neuroprotective effect.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

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

描述CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively. Leucine-rich repeat kinase 2 (LRRK2) is a large and complex protein, with multiple enzymatic and protein-interaction domains, each of which is effected by mutations^[3]. CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ~1 to ~5 Nm, while the G2019S mutant was inhibited with an IC50 ranging from ~2 to ~7 nM in a TF-FRET assay. LRRK2 mutations were observed in sporadic as well as familial parkinson's disease (PD)patients and have been investigated intensively, and the most common mutation in PD patients is G2019S^[3]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-54252 with an EC50 of ~1 nM and fully reversed to wild-type levels at concentration as low as 1.6 nM for CZC-54252^[4]. Unfortunately, it failed to cross the blood–brain barrier (BBB), displaying only 4% BBB penetration^[4].
参考文献

[1] Kramer T, Lo Monte F, et al. Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models. ACS Chem Neurosci. 2012 Mar 21;3(3):151-60.
[2] Ramsden N, Perrin J, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.
[3] Kramer T, Lo Monte F, Göring S, Okala Amombo GM, Schmidt B. Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models. ACS Chem Neurosci. 2012 Mar 21;3(3):151-60. doi: 10.1021/cn200117j. Epub 2012 Jan 18. PMID: 22860184; PMCID: PMC3369800.
[4] Ramsden N, Perrin J, Ren Z, Lee BD, Zinn N, Dawson VL, Tam D, Bova M, Lang M, Drewes G, Bantscheff M, Bard F, Dawson TM, Hopf C. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. doi: 10.1021/cb2002413. Epub 2011 Aug 10. PMID: 21812418; PMCID: PMC3688284.

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
- 1.9802 mL
- 9.9012 mL
- 19.8024 mL
- 5 mM
- 0.3960 mL
- 1.9802 mL
- 3.9605 mL
- 10 mM
- 0.1980 mL
- 0.9901 mL
- 1.9802 mL

技术信息

CAS号

1191911-27-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H25ClN6O4S

运输

蓝冰

分子量

504.99

别名

CZC-54252

溶解度

DMSO	210.0 mg/mL (415.9 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

CZC-54252 Catalog No. CSN16309

靶点选择性

请登录您的专属账户

确认信息