HG-10-102-01
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更新时间: 2026-01-19 17:16:39
CAS号:1351758-81-0
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纯度: 99.0%
备货期: 10天
库存: 现货
其他详情(用途,包装):
用途: HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM)IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1]Target: LRRK2HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2. HG-10-102-01 exhibited biochemical IC50s of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. At a concentration of 10 μM, HG-10-102-01 only inhibited the kinase activities of MLK1 and MNK2 to greater than 80% of the DMSO control. Dose-response analysis revealed inhibition of MLK1 with an IC50 2.1 μM and MNK2 with an IC50 0.6 μM. KinomeScan analysis against a near comprehensive panel of 451 kinases at a concentration of 1 μM resulted in no interactions detected with kinases other than G2019S LRRK2 with the exception of one mutant form of c-Kit (L576P) demonstrating the outstanding selectivity of this inhibitor.HG-10-102-01 significantly inhibited phosphorylation of wildtype LRRK2 and LRRK2[G2019S] mutant at Ser910 and Ser935 at 0.3-1.0 μM in cell culture, which is approximately the same potency as LRRK2-IN-1 (1). HG-10-102-01 is relatively insensitive to the A2016T mutation which suggests that this mutant will not be useful to validate whether the pharmacological effects of the compound are LRRK2-dependent.HG-10-102-01 can inhibit phosphorylation of Ser910 and Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 50 mg/kg. Further optimization of this chemo-type especially in regards to in vivo half-life will be reported in due course [1]. 物理化学性质: CAS号:1351758-81-0 常用中文名:[4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮 常用英文名:HG-10-102-01 分子式:C17H20ClN5O3 分子量:377.825 密度:1.4±0.1 g/cm3 沸点:641.1±65.0 °C at 760 mmHg 熔点:N/A 闪点:341.5±34.3 °C 储存条件:2-8℃
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公司名:上海念兴实业有限公司 推荐
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商品数: 403768件
电话: 18916513247
地址: 2222 Huancheng Road, Juyuan New District, Jiading District, Shanghai
地区: 上海市普陀区
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联系人电话: 0086-021-52280163
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公司名:上海阿拉丁生化科技股份有限公司
区域:上海市浦东新区
价格:
¥1019.9/5mg
¥7580.9/100mg
¥1632.9/10mg
¥2966.9/25mg
联系人:阿拉丁
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HG-10-102-01价格为, 由HG-10-102-01生产厂家上海念兴实业有限公司提供,供应信息包括纯度,备货期/库存,供货能力等。>>电脑版:HG-10-102-01_价格_生产厂家【上海念兴实业有限公司】
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