S82263 |
CZC-54252 |
源叶(MedMol) | ≥98% |
- 提示:详情请下载说明书。
- 产品描述: CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity
- 靶点: IC50: 1.28 nM (Wild-type LRRK2) and 1.85 nM (G2019S LRRK2);LRRK2
- 体外研究:
CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ~1 to ~5 nM. The G2019S mutant is inhibited with an IC50 ranging from ~2 to ~7 nM in a TF-FRET assay. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC50 of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM
- 参考文献:
1. Ramsden N, 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.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.98 ml 9.901 ml 19.802 ml 5 mM 0.396 ml 1.98 ml 3.96 ml 10 mM 0.198 ml 0.99 ml 1.98 ml 50 mM 0.04 ml 0.198 ml 0.396 ml
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