| 常用名 | CZC-54252 | CAS号 | 1191911-27-9 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情(用途,包装等)
用途: 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.IC50 value: 1.28 nM/1.85 nM(LRRK2/G2019S LRRK2) [1]Target: LRRK2 inhibitorin vitro: CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ~1 to ~5 nM. The G2019S mutant was inhibited with an IC50 ranging from ~2 to ~7 nM in a TF-FRET assay. In addition, they were screened against a kinase panel of 185 kinases and exhibited good selectivity. CZC-25146 (19) inhibited five other kinases, PLK4, GAK, TNK1, CAMKK2, and PIP4K2C, with high potency only, but none of them have been classified as predictors of genotoxicity or hematopoietic toxicity [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) [2].in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146 (19). Unfortunately, it exhibited a poor brain penetration of just 4%. 物理化学性质: CAS号:1191911-27-9 常用中文名:CZC-54252 常用英文名:CZC-54252 分子式:C22H25ClN6O4S 分子量:504.990 密度:1.5±0.1 g/cm3 沸点:718.1±70.0 °C at 760 mmHg 熔点:N/A 闪点:388.1±35.7 °C 储存条件:-20℃ |