| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S88364-1mg买3赠1 |
99.90% | ￥200.00 |
9 | - | - | - | - |
|
S88364-5mg买3赠1 |
99.90% | ￥490.00 |
5 | - | - | - | - |
|
S88364-10mg买3赠1 |
99.90% | ￥760.00 |
6 | - | - | - | - |
|
S88364-25mg促销 |
99.90% | ￥1550.00 ￥1240.00 |
6 | - | - | - | - |
|
S88364-50mg促销 |
99.90% | ￥2290.00 ￥1830.00 |
5 | - | - | - | - |
|
| 产品描述： | HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research | ||||||||||||||||||||
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| 靶点： | IC50: 3.2 nM (LRRK2[G2019S]), 20.3 nM (wild-type LRRK2), 95.9 nM (LRRK2[G2019S+A2016T], 153.7 nM (LRRK2[A2016T]), 0.6 μM (MNK2), 2.1 μM (MLK1);LRRK2 | ||||||||||||||||||||
| 体内研究： | HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice. HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure. Animal Model: Wild type male C57BL/6 mice Dosage: 0, 3, 10, 30, 50, and 100 mg/kg Administration: IP, once Result: Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses. | ||||||||||||||||||||
| 参考文献： | 1. Choi HG, et al. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. 2. Wang M, et al. Synthesis of [11C]HG-10-102-01 as a new potential PET agent for imaging of LRRK2 enzyme in Parkinson's disease. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1351-1355. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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北京