产品
编 号:F254223
分子式:C25H39ClN4O3
分子量:479.06
产品类型
结构图
CAS No: 2070015-25-5
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产品详情
生物活性:
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.
体内研究:
EPZ020411 hydrochloride (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model.1.19Pharmacokinetic Parameters of EPZ020411 hydrochloride in rats.RatsIV 1 mg/kg RatsSC 5 mg/kg
CL (mL/min/kg)19.7±1.0
Vss (L/kg)11.1±1.6
t1/2 (h)8.54±1.439.19±1.60
tmax (h)0.444
Cmax (ng/mL)844±306
AUC0-τ (h·ng/mL)745±342456±135
AUC0-inf (h·ng/mL)846±452775±181
F (%)65.6±4.3
Animal Model:C57BL/6J wild-type mice at P28 with acute ototoxicity model
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg once
Result:Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
体外研究:
EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells.EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival.