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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 40 In Stock
5MG 61 In Stock
10MG 105 In Stock
25MG 228 In Stock
50MG 412 In Stock
100MG 606 In Stock
500MG 1287 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    CZC-25146
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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.
  • In Vitro
    CZC-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.
  • In Vivo
    CZC-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.
  • Synonyms
    ——
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    G2019S LRRK2| LRRK2
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    1191911-26-8
  • Formula Weight
    488.54
  • Molecular Formula
    C22H25FN6O4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 46 mg/mL; 94.16 mM
  • SMILES
    COc1c(ccc(c1)N1CCOCC1)Nc1ncc(c(n1)Nc1ccccc1NS(=O)(=O)C)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ramsden N, et al. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.
molnova catalog
related products
  • mTOR inhibitor 9c

    mTOR inhibitor 9c is a selective mTOR inhibitor with IC50 of 0.7nM and 825nM for mTOR and PI3Kα, respectively.

  • MTI-31

    MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR).

  • JR-AB2-011

    JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.