CZC-25146 MedChemExpress (MCE)

Product Name	CZC-25146
Synonyms	CZC25146 CZC 25146 CZC-25146 CHEMBL2397014 LRRK2 INHIBITOR II LRRK2 Inhibitor II N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide Synonyms CZC25146 CZC 25146 CZC-25146 CHEMBL2397014 LRRK2 INHIBITOR II LRRK2 Inhibitor II N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide N-(2-((5-fluoro-2-((2-methoxy-4- morpholinophenyl)amino)pyrimidin- 4- yl)amino)phenyl)methanesulfonamide N-[2-[[5-Fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide Methanesulfonamide, N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-
CAS	1191911-26-8
EINECS
Chemical Formula	C22H25FN6O4S
Molecular Weight	488.54
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Get quote
Descriptions	CZC-25146 CZC-25146 MedChemExpress (MCE) HY-15800A 1191911-26-8 99.10% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions CZC-25146 CZC-25146 MedChemExpress (MCE) HY-15800A 1191911-26-8 99.10% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases. CZC-25146 (0.01-5 μM 7 days) does not cause cytotoxicity in human cortical neurons, nor blocking neuronal development[1]. CZC-25146 (0.01-5 μM 2 days) potently attenuates G2019S LRRK2-mediated toxicity in primary rodent neurons in a concentration-dependent manner with an EC50 of ~100 nM[1]. CZC-25146 (0.06-1000 nM) rescues LRRK2 G2019S-induced neurite defects in primary human neurons in a dose-dependent manner[1]. CZC-25146 (14.3 and 28.6 μM 48 h) markedly reduces The mutant AAT encoded by the Z allele (ATZ) polymer load and restores AAT secretion in iPSC-Hepatocyte, without compromising cell viability[3]. CZC-25146 (250 mg/kg p.o. 14 days) reduces the ATZ polymer levels in over expressing human polymeric ATZ mice[3]. CZC-25146 (1 mg/kg for i.v. 5 mg/kg for p.o. single dosage) exhibits relatively good pharmacokinetic properties and an extensive distribution throughout animal body following intravenous injection into mice[1]. IC50: 4.76 nM (wild-type LRRK2), 6.87 nM (G2019S LRRK2)[1] In Vitro CZC-25146 (0.01-5 μM 7 days) does not cause cytotoxicity in human cortical neurons, nor blocking neuronal development[1]. CZC-25146 (0.01-5 μM 2 days) potently attenuates G2019S LRRK2-mediated toxicity in primary rodent neurons in a concentration-dependent manner with an EC50 of ~100 nM[1]. CZC-25146 (0.06-1000 nM) rescues LRRK2 G2019S-induced neurite defects in primary human neurons in a dose-dependent manner[1]. CZC-25146 (14.3 and 28.6 μM 48 h) markedly reduces The mutant AAT encoded by the Z allele (ATZ) polymer load and restores AAT secretion in iPSC-Hepatocyte, without compromising cell viability[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CZC-25146 Related Antibodies Cell Cytotoxicity Assay[1] Cell Line: Human cortical neurons \| \| \| \| \| \| \| \| \| \| [1]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21 6(10):1021-8. [Content Brief] [2]. Atashrazm F, et al. LRRK2 inhibitors and their potential in the treatment of Parkinson's disease: current perspectives. Clin Pharmacol. 2016 Oct 20 8:177-189. [Content Brief] [3]. Deniz Kent, et al. Small molecule screen employing patient-derived iPS hepatocytes identifies LRRK2 as a novel therapeutic target for Alpha1 Antitrypsin Deficiency.
Last Update	2025-04-01 14:45:47

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