EPZ020411

COA

级别和纯度:

Moligand™

CAS编号: 1700663-41-7
分子式: C₂₅H₃₈N₄O₃
分子量: 442.6
PubChem编号: 91668547

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货号 (SKU)	包装规格	是否现货
E647956-5mg	5mg	期货
E647956-10mg	10mg	期货
E647956-50mg	50mg	期货

查看相关系列

Apoptosis (7108) Histone Modification (3105) 组蛋白甲基转移酶 (190) 表观遗传学 (1497)

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基本描述

规格或纯度	Moligand™
英文名称	EPZ020411
生化机理	EPZ020411 是 PRMT6 的选择性抑制剂，IC 50 为 10 nM，对 PRMT6 的选择性大于 PRMT1 和 PRMT8 的 10 倍。EPZ020411 可用于癌症研究。
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	抑制剂
产品介绍	EPZ020411 is a selective inhibitor of PRMT6 with an IC 50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8 . EPZ020411 can be used for the research of cancer In Vitro EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells. EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: A375 cells Concentration: 0-20 μM Incubation Time: 24 hours Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC 50 of 0.634 μM. Apoptosis AnalysisCell Line: Cultured cochleae cells Concentration: 20-40 μM Incubation Time: 6 hours Result: Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Also reduced hair cell loss caused by cisplatin treatment. In Vivo EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model. 1.19 Pharmacokinetic Parameters of EPZ020411 in rats . Rats IV 1 mg/kg Rats SC 5 mg/kg CL (mL/min/kg) 19.7±1.0 V ss (L/kg) 11.1±1.6 t 1/2 (h) 8.54±1.43 9.19±1.60 t max (h) 0.444 C max (ng/mL) 844±306 AUC 0-τ (h·ng/mL) 745±34 2456±135 AUC 0-inf (h·ng/mL) 846±45 2775±181 F (%) 65.6±4.3 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity modelDosage: 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. IC50& Target:PRMT6 0.01 μM (IC 50 ) PRMT1 0.119 μM (IC 50 ) PRMT8 0.223 μM (IC 50 )

关联靶点（人）

PRMT6 Tchem 蛋白质精氨酸N-甲基转移酶6(Protein arginine N-methyltransferase 6) (1 活性数据)

点击查看靶蛋白信息： PRMT6

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

IIUPAC Name	N,N'-dimethyl-N'-[[5-[4-[3-[2-(oxan-4-yl)ethoxy]cyclobutyl]oxyphenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine
INCHI	1S/C25H38N4O3/c1-26-10-11-29(2)18-21-17-27-28-25(21)20-3-5-22(6-4-20)32-24-15-23(16-24)31-14-9-19-7-12-30-13-8-19/h3-6,17,19,23-24,26H,7-16,18H2,1-2H3,(H,27,28)
InChi Key	QMDKVNSQXPVCRD-UHFFFAOYSA-N
Smiles	CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4
Isomeric SMILES	CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4
PubChem CID	91668547
分子量	442.6

化学和物理性质

分子量	442.600 g/mol
XLogP3	2.700
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	6
可旋转键计数Rotatable Bond Count	12
精确质量Exact Mass	442.294 Da
单同位素质量Monoisotopic Mass	442.294 Da
拓扑极表面积Topological Polar Surface Area	71.600 Å²
重原子数Heavy Atom Count	32
形式电荷Formal Charge	0
复杂度Complexity	519.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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