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URMC-099 是一种具有优异的血脑屏障穿透性的,可口服的混合谱系激酶 3 抑制剂,IC50为14 nM。
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URMC-099 是一种具有优异的血脑屏障穿透性的,可口服的混合谱系激酶 3 抑制剂,IC50为14 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 349 | 现货 | |
5 mg | ¥ 816 | 现货 | |
10 mg | ¥ 1,230 | 现货 | |
25 mg | ¥ 2,150 | 现货 | |
50 mg | ¥ 3,320 | 现货 | |
100 mg | ¥ 4,920 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 816 | 现货 |
产品描述 | URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM). |
靶点活性 | MLK2:42nM, DLK:150 nM, MLK1:19nM, MLK3:14nM |
体外活性 | URMC-099(10 mg/kg, i.p. )可减少体内炎性细胞因子产生,保护神经元结构,并改变小胶质细胞对HIV-1 Tat暴露下的形态和超微响应.URMC-099在小鼠体内,表现出良好的药代动力学性能和改善的CNS渗透性.URMC099明显减少野生型小鼠体内中性粒细胞通过fMLP进入腹膜. |
体内活性 | URMC-099可降低体外实验中fMLP诱导的野生型嗜中性粒细胞的趋药性。URMC-099还对小胶质细胞中脂多糖诱导的TNFα释放,以及人单核细胞中HIV-1 Tat诱导的细胞因子释放有抑制作用。 URMC-099防止培养的神经轴突被小胶质细胞破坏和吞噬。 |
激酶实验 | HDAC IC50 Profiling: The in vitro inhibitory activity of compounds against seven human HDAC isoforms (1, 2, 4 C2A, 5 C2A, 6, 8, and 11) are performed with a fluorescent based assay according to the company's standard operating procedure. The IC50 values are determined using 10 different concentrations with 3-fold serial dilution starting at 10 μM. TSA and vorinostat are used as reference compounds. |
分子量 | 421.54 |
分子式 | C27H27N5 |
CAS No. | 1229582-33-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 6 mg/mL (14.2 mM) DMSO: 75 mg/mL (177.9 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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