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CZC-25146

Catalog No.GC16038

LRRK2 inhibitor

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CZC-25146 Chemical Structure

Cas No.: 1191911-26-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$116.00
In stock
10mg
$114.00
In stock
100mg
$916.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

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
Solubility ≥ 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.

Complete Stock Solution Preparation Table

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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
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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