CZC-25146
目录号 : GC16038
A potent LRRK2 inhibitor
Cas No.:1191911-26-8
Sample solution is provided at 25 µL, 10mM.
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CZC-25146 is a selective and cell-penetrant inhibitor of leucine-rich repeat kinase-2 (LRRK2) with IC50 value of 4.76nM [1].
CZC-25146 is a second generation inhibitor of LRRK2 with excellent potency and selectivity. In a time-resolved fluorescence resonance energy transfer assay, CZC-25146 shows potent inhibition of both recombinant human wild type LRRK2 and G2019S mutant LRRK2 with IC50 values of 4.76nM and 6.87nM, respectively. CZC-25146 is selective against LRRK2. When treated with 184 different protein kinases and one lipid kinase, CZC-25146 inhibits only five of them with high potency including PLK4, GAK, TNK1, CAMKK2 and PIP4K2C. Besides that, CZC-25146 is found to relieve the G2019S LRRK2-induced cell injury and death with EC50 value of 100nM in neurons of primary rodent cortical. It also attenuates G2019S LRRK2-induced human neuronal injury with EC50 value of 4nM. However, CZC-25146 lacks sufficient brain exposure to be used in rodent models of PD [1, 2].
References:
[1] Ramsden N, Perrin J, Ren Z, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson’s disease-related toxicity in human neurons. ACS chemical biology, 2011, 6(10): 1021-1028.
[2] Troxler T, Greenidge P, Zimmermann K, et al. Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2. Bioorganic & medicinal chemistry letters, 2013, 23(14): 4085-4090.
| Cas No. | 1191911-26-8 | SDF | |
| 化学名 | (E)-N-(2-((5-fluoro-2-((2-methoxy-4-morpholinophenyl)amino)pyrimidin-4(3H)-ylidene)amino)phenyl)methanesulfonamide | ||
| Canonical SMILES | COC1=C(NC2=NC=C(F)/C(N2)=N\C3=CC=CC=C3NS(C)(=O)=O)C=CC(N4CCOCC4)=C1 | ||
| 分子式 | C22H25FN6O4S | 分子量 | 488.54 |
| 溶解度 | ≥ 24.45mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.0469 mL | 10.2346 mL | 20.4692 mL |
| 5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL |
| 10 mM | 0.2047 mL | 1.0235 mL | 2.0469 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet