Chemical Structure : MLi-2
CAS No.: 1627091-47-7
货号: PC-21889Not For Human Use, Lab Use Only.
MLi-2 is a potent, highly selective, orally available, brain-penetrant inhibitor of LRRK2 with IC50 of 0.76 nM, pSer935 LRRK2 IC50 of 1.4 nM.
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|---|---|---|---|
| 2 mg | ¥780 | In stock | |
| 5 mg | ¥1180 | In stock | |
| 10 mg | ¥1780 | In stock | |
| 25 mg | ¥2980 | In stock | |
| 50 mg | ¥4580 | In stock | |
| 100 mg | Get quote |
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MLi-2 is a potent, highly selective, orally available, brain-penetrant inhibitor of LRRK2 with IC50 of 0.76 nM, pSer935 LRRK2 IC50 of 1.4 nM.
MLi-2 shows an IC50 of 3.4 nM in a radioligand competition binding assay, > 95-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels.
MLi-2 signficantly reduces the ratio of phosphorylated Ser935 LRRK2 (pS935) to total LRRK2 in the mouse cortex in both single dose and 11-day in-diet studies.
MLi-2 significantly reduces pS935 in a dose dependent manner (1–100 mg/kg) 1 h post treatment in rats.
| 分子量 | 379.46 | |
| 分子式 | C21H25N5O2 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
rel-(2S,6R)-2,6-Dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine |
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1. Scott JD, et al. J Med Chem. 2017 Apr 13;60(7):2983-2992.
2. Fell MJ, et al. J Pharmacol Exp Ther. 2015 Dec;355(3):397-409.
3. Volpicelli-Daley LA, et al. J Neurosci. 2016 Jul 13;36(28):7415-27.
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