| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M408789-1ml |
1ml |
现货  |
|
| 英文别名 | 1H-Indazole, 3-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-pyrimidinyl]-5-[(1-methylcyclopropyl)oxy]-, rel- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | MLi-2 |
| 生化机理 | MLi-2 是一种口服活性高选择性 LRRK2 抑制剂。在体外纯化 LRRK2 激酶测定中，MLi-2 表现出卓越的效力，IC50 为 0.76 nM；在细胞测定中，MLi-2 监测 LRRK2 pSer935 LRRK2 的去磷酸化，IC50 为 1.4 nM；在放射性配体竞争结合测定中，IC50 为 3.4 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 富亮氨酸重复激酶 2 抑制剂 |
| 产品介绍 |
MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂，具有中枢神经系统活性，IC50为 0.76 nM，有潜力用于帕金森氏病。
Information MLi-2 MLi-2 is an orally active and highly selective inhibitor of LRRK2 . MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 o MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM). MLi-2 has greater than 295-fold selectivity for over 300 kinases in addition to a diverse panel of receptors and ion channels. In vivo Acute oral and subchronic dosing in MLi-2 mice resulted in dosedependent central and peripheral target inhibition over a 24-hour period as measured by dephosphorylation of pSer935 LRRK2. Treatment of MitoPark mice with MLi-2 is well tolerated over a 15-week period at brain and plasma exposures >100× the in vivo plasma IC50 for LRRK2 kinase inhibition as measured by pSer935 dephosphorylation. Morphologic changes in the lung, consistent with enlarged type II pneumocytes, are observed in MLi-2-treated MitoPark mice. cell lines：U87-MG, T98G, and U373-MG Concentrations：10 serial 3-fold dilutions, top concentration 5 μM Incubation Time：90 min Powder Purity:≥98% |
| ALogP | 3.892 |
|---|---|
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 4 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1CN(CC(C)O1)C2=CC(=NC=N2)C3=N[NH]C4=CC=C(OC5(C)CC5)C=C34 |
| 分子量 | 379.46 |
| Reaxy-Rn | 35816280 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35816280&ln= |
| DMSO(mg / mL) Max Solubility | 76 |
|---|---|
| DMSO(mM) Max Solubility | 200.28 |
| Water(mg / mL) Max Solubility | 76 |
| Water(mM) Max Solubility | 200.28 |
| Reaxy-Rn | 35816280 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=35816280&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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