| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87766-5mg促销 |
98% | ￥506.00 ￥455.00 |
10 | - | - | - | - |
|
S87766-10mg促销 |
98% | ￥912.00 ￥820.00 |
10 | - | - | - | - |
|
S87766-25mg促销 |
98% | ￥1580.00 ￥1420.00 |
6 | - | - | - | - |
|
S87766-50mg促销 |
98% | ￥2840.00 ￥2560.00 |
2 | - | - | - | - |
|
S87766-100mg促销 |
98% | ￥6380.00 ￥5750.00 |
2 | - | - | - | - |
|
| 产品描述： | JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome | ||||||||||||||||||||
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| 靶点： | LRRK2 | ||||||||||||||||||||
| 体外研究： | JH-II-127 (0.03, 0.1, 0.3, 1, 3 µM; 90 min) inhibits LRRK2 in HEK293 cells. JH-II-127 (0.3, 1, 3 µM; 90 min) inhibits endogenously expressed LRRK2 in mouse Swiss 3T3 cells. Western Blot Analysis Cell Line: HEK293 cells (expressing GFP-LRRK2, GFP-LRRK2[G2019S], GFP-LRRK2[G2019S + A2016T], and GFP-LRRK2[A2016T], respectively) Concentration: 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 90 min Result: Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells.Inhibited phosphorylation of Ser910 and Ser935 at approximately 0.3 μM for wild-type LRRK2 and LRRK2[G2019S].Induced dephosphorylation of Ser910 and Ser935 at a concentration of 0.3-1 μM in the drug-resistant LRRK2[A2016T + G2019S] and LRRK2[A2016T] mutants. Western Blot Analysis Cell Line: Mouse Swiss 3T3 cells Concentration: 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 90 min Result: Induced similar dose-dependent Ser935 dephosphorylation of endogenous LRRK2. | ||||||||||||||||||||
| 体内研究： | JH-II-127 (100 mg/kg; i.p.; single) results in near complete dephosphorylation of Ser935 of LRRK2 in all tissues including brain | ||||||||||||||||||||
| 参考文献： | 1. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-9. | ||||||||||||||||||||
| 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