CZC-25146 |
| カタログ番号GC16038 |
CZC-25146 は、野生型 LRRK2 および G2019S LRRK2 に対してそれぞれ 4.76 nM および 6.87 nM の IC50 値を持つ強力な経口活性 LRRK2 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | (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 | ||
| Formula | C22H25FN6O4S | M.Wt | 488.54 |
| 溶解度 | ≥ 24.45mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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