
CZC-25146
CAS No. 1191911-26-8
CZC-25146( —— )
Catalog No. M17181 CAS No. 1191911-26-8
CZC-25146 is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 40 | In Stock |
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5MG | 61 | In Stock |
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10MG | 105 | In Stock |
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25MG | 228 | In Stock |
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50MG | 412 | In Stock |
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100MG | 606 | In Stock |
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500MG | 1287 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameCZC-25146
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NoteResearch use only, not for human use.
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Brief DescriptionCZC-25146 is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.
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DescriptionCZC-25146 is an effective, specific and metabolically stable LRRK2 inhibitor with IC50 of 4.76/6.87 nM for wild-type LRRK2(Leucine-rich repeat kinase-2) and G2019S LRRK2, respectively.
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In VitroCZC-25146 (0.01-5 μM; 7 days) does not cause cytotoxicity in human cortical neurons, nor blocking neuronal development.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.CZC-25146 (0.06-1000 nM) rescues LRRK2 G2019S-induced neurite defects in primary human neurons in a dose-dependent manner. 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. Cell Cytotoxicity Assay Cell Line:Human cortical neurons Concentration:0.01, 0.1, 1 and 5 μM Incubation Time:7 days Result:Did not cause cytotoxicity in human cortical neurons at concentrations below 5 μM over a seven-day treatment in culture, nor did it block neuronal development.
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In VivoCZC-25146 (250 mg/kg; p.o.; 14 days) reduces the ATZ polymer levels in over expressing human polymeric ATZ mice.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. Animal Model:Genetically modified male mice (6 weeks; over expressing human polymeric ATZ)Dosage:250 mg/kg Administration: p.o.; 14 days Result:Dramatically and reproducibly reduced the ATZ polymer levels with an overall reduction from 60% in the control group to 37%.Animal Model:Male CD-1 mice Dosage:1 mg/kg for i.v.; 5 mg/kg for p.o.Administration:i.v. and p.o.; single dosage Result:Pharmacokinetic Parameters of CZC-25146 in male CD-1 mice.
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Synonyms——
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PathwayPI3K/Akt/mTOR signaling
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TargetmTOR
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RecptorG2019S LRRK2| LRRK2
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number1191911-26-8
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Formula Weight488.54
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Molecular FormulaC22H25FN6O4S
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 46 mg/mL; 94.16 mM
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SMILESCOc1c(ccc(c1)N1CCOCC1)Nc1ncc(c(n1)Nc1ccccc1NS(=O)(=O)C)F
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Ramsden N, et al. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.
molnova catalog



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