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

CZC-25146 hydrochloride 是一种有效且具有口服活性的 LRRK2 抑制剂，对野生型 LRRK2 和突变型 LRRK2 G2019S 的 IC50 分别为 4.76 nM 和 6.87 nM，也抑制激酶 PLK4、GAK、TNK1、CAMKK2 和 PIP4K2C。CZC-25146 hydrochloride 能在体外抑制突变 LRRK2 诱导的神经元损伤。CZC-25146 hydrochloride 在小鼠体内表现出相对较好的药代动力学特性。CZC-25146 hydrochloride 还能增加正常的 α-1 抗胰蛋白酶 (AAT) 的分泌，减少炎症细胞因子。CZC-25146 hydrochloride 可用于帕金森病和肝病的研究。

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CZC-25146 hydrochloride Chemical Structure

CZC-25146 hydrochloride Chemical Structure

CAS No. : 1330003-04-7

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CZC-25146 hydrochloride 的其他形式现货产品:

Other Forms of CZC-25146 hydrochloride:

CZC-25146 hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(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].

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

CZC-25146 hydrochloride 相关抗体:

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.
体内研究
(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].

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%
分子量

525.00

Formula

C22H26ClFN6O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CZC-25146 hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

CZC-251461330003-04-7CZC25146CZC 25146LRRK2Leucine-rich repeat kinase 2LRRK2 G2019Sneuronsα-1-antitrypsininflammatoryParkinson's diseaseliver diseasesInhibitorinhibitorinhibit

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