产品说明书
CZC-54252
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同义名 : | - |
| CAS号 : | 1191911-27-9 | |
| 货号 : | A408166 | |
| 分子式 : | C22H25ClN6O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 504.99 | |
| MDL号 : | MFCD26401527 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(207.93 mM)，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 |
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| 动物实验配方： |
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.98mL 0.40mL 0.20mL |
9.90mL 1.98mL 0.99mL |
19.80mL 3.96mL 1.98mL |
| 参考文献 |
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