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DN-1289 是一种可口服可通过血脑屏障且具有选择性高效性的抑制剂,对双亮氨酸拉链激酶 (DLK)的 IC50 值为17 nM,对 亮氨酸拉链轴承激酶 (LZK)的 IC50 值为 40 nM。DN-1289 对小鼠模型中视神经挤压 (ONC) 诱导的 p-c-Jun 有显著的抑制作用。
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DN-1289 是一种可口服可通过血脑屏障且具有选择性高效性的抑制剂,对双亮氨酸拉链激酶 (DLK)的 IC50 值为17 nM,对 亮氨酸拉链轴承激酶 (LZK)的 IC50 值为 40 nM。DN-1289 对小鼠模型中视神经挤压 (ONC) 诱导的 p-c-Jun 有显著的抑制作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 2,350 | 现货 | |
5 mg | ¥ 7,000 | 现货 | |
10 mg | ¥ 8,550 | 现货 | |
25 mg | ¥ 11,240 | 现货 | |
50 mg | ¥ 13,800 | 现货 | |
100 mg | ¥ 17,500 | 现货 |
产品描述 | DN-1289 is an orally available, blood-brain barrier-crossing, selective and potent inhibitor with an IC50 value of 17 nM for di-leucine zipper kinase (DLK) and 40 nM for leucine zipper-bearing kinase (LZK).DN-1289 significantly inhibited optic nerve crush (ONC)-induced p-c-Jun in a mouse model. |
体外活性 | DN-1289 (Compound 14) (0.1, 0.3, and 1 μM; 0-20 h) can block the neurite degeneration induced by nerve growth factor (NGF) withdrawal in dorsal root ganglion (DRG) neurons[1]. DN-1289 (0.1, 0.3, and 1 μM; 0-20 h) inhibits the activation of caspases, apoptotic protease, in NGF withdrawal-induced apoptosis in DRG neurons[1]. |
体内活性 | DN-1289 (Compound 14) demonstrates good tolerance in a mouse model at doses of 100 mg/kg and 150 mg/kg administered via intraperitoneal injection once daily for 10-15 days[1]. DN-1289 (150 mg/kg; oral administration; twice daily for 10 days) inhibits c-Jun phosphorylation in the acute optic nerve crush (ONC) injury model[1]. |
分子量 | 441.38 |
分子式 | C18H19F4N7O2 |
Smiles | NC1=C(OC(F)F)N=C(C2=NC(N3[C@@H]4CO[C@H](C3)C4)=NC(N5CC(F)(CC5)F)=C2)C=N1 |
存储 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (124.61 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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