1. Autophagy
  2. LRRK2
  3. CZC-25146 hydrochloride

CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.

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CZC-25146 hydrochloride Chemical Structure

CZC-25146 hydrochloride Chemical Structure

CAS No. : 1330003-04-7

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Description

CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases[1][2][3].

IC50 & Target

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.

Cell Cytotoxicity Assay[1]

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 (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].
CZC-25146 (250 mg/kg; p.o.; 14 days) reduces the ATZ polymer levels in over expressing human polymeric ATZ mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice[1]
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[1].
i.v. (1 mg/kg) p.o. (5 mg/kg)
CL (L/h/kg) 2.3
Vss (L/kg) 5.4
t1/2 (h) 1.6 1
tmax (h) 0 0.25
Cmax (ng/mL) 154 1357
AUClast (ng/mL·h) 419 2878
AUCinf (ng/mL·h) 434 2894
F (%) 133
Animal Model: Genetically modified male mice (6 weeks; over expressing human polymeric ATZ)[3]
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%
Molecular Weight

525.00

Formula

C22H26ClFN6O4S

CAS No.
SMILES

CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2F)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CZC-25146 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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