DN-1289
目录号 : GC71195DN-1289是一种口服活性和选择性的双亮氨酸拉链激酶（DLK；IC50=17 nM）和亮氨酸拉链携带激酶（LZK；IC5=40 nM）抑制剂。
Cas No.:3026597-15-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability.
DN-1289 (compound 14) (0.1, 0.3, and 1 μM; 0-20 h) can block axon degeneration in dorsal root ganglion (DRG) neurons induced by nerve growth factor (NGF) withdrawal[1].
DN-1289 (0.1, 0.3, and 1 μM; 0-20 h) inhibits the activation of caspases in DRG neurons over time induced by NGF withdrawal[1].
DN-1289 (compound 14) (100 mg/kg and 150 mg/kg; i.p.; once daily for 10-15 d) is well-tolerated in mice model[1].
DN-1289 (150 mg/kg; p.o.; b.i.d. for 10 d) inhibits phosphorylation of c-Jun in an acute injury model with optic nerve crush (ONC) application[1].
Pharmacokinetic Analysis[1]
| Species | Route | Dose (mg/kg) | plasma Cmax (μM) | plasma AUC0-24 h (μM·h) | CLp (mL/min/kg) | CLu (mL/min/kg) | Vd (L/kg) | t1/2 (h) | F (%) | Kpuu (AUC) | brain AUC0-2 h (μM·h) |
| rat | IV | 1 | 1.09 | 2.42 | 14.7 | 150 | 6.7 | 6.5 | / | 0.6 | 4.05 |
| PO | 3 | 0.58 | 3.9 | / | / | / | 4.6 | 52 | / | / | |
| mouse | IV | 1 | 1.06 | 4.06 | 8.6 | 200 | 4.7 | 6.8 | / | / | / |
| PO | 10 | 2.32 | 21.9 | / | / | / | 7.9 | 56 | 0.4 | 6.91 | |
| PO | 150 | 24.9 | 324 | / | / | / | 23.7 | 53 | / | / | |
| IP | 100 | 15.4 | 280 | / | / | / | 23.7 | 53 | / | / | |
| cyno | IV | 0.5 | 0.746 | 2.79 | 6.1 | 64 | 3.4 | 7.9 | / | / | / |
GLPBIO has not independently confirmed the accuracy of these methods. They are for reference only.
References:
[1]. Craig RA 2nd, et al. Discovery of Potent and Selective Dual Leucine Zipper Kinase/Leucine Zipper-Bearing Kinase Inhibitors with Neuroprotective Properties in In Vitro and In Vivo Models of Amyotrophic Lateral Sclerosis. J Med Chem. 2022 Dec 22;65(24):16290-16312.
| Cas No. | 3026597-15-6 | SDF | |
| 分子式 | C18H19F4N7O2 | 分子量 | 441.38 |
| 溶解度 | 储存条件 | ||
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2656 mL | 11.3281 mL | 22.6562 mL |
| 5 mM | 0.4531 mL | 2.2656 mL | 4.5312 mL |
| 10 mM | 0.2266 mL | 1.1328 mL | 2.2656 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。