N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride
CAS: 2070015-25-5
Molecular Formula: C25H39ClN4O3
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride - Names and Identifiers
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride - Physico-chemical Properties
| Molecular Formula | C25H39ClN4O3 |
| Molar Mass | 479.05516 |
| Storage Condition | 2-8℃ |
| Target | PRMT6 |
| In vitro study | In human melanoma A375 cells exogenously overexpressing PRMT6, EPZ020411 dose-dependently reduced H3R2 methylation (IC50=0.637±0.241 μm). In biochemical assays, EPZ020411 was more selective for PRMT6/8/1 than for other histone methyltransferases (including 4 arginine methyltransferases PRMT3, PRMT4, PRMT5, PRMT7) more than 100 times higher. In the parallel artificial membrane permeation test, EPZ020411 has poor permeability. |
| In vivo study | EPZ020411 has good bioavailability by subcutaneous injection in rats and is a suitable compound for in vivo studies. A single intravenous injection of 1 mg/kg EPZ020411 into male Sprague-Dawley rats resulted in an in vivo clearance (CL) of 19.7±1.0 mL/min/kg and a volume of distribution (Vss) at steady state was 11.1±1.6 L/kg with an average half-life of 8.54±1.43 h. With subcutaneous injection of 5 mg/kg, with good bioavailability 65.6±4.3%, the free concentration of EPZ020411 in the blood was higher than the biochemical IC50 value of PRMT6 for more than 12 hours. |
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.087 ml | 10.437 ml | 20.874 ml |
| 5 mM | 0.417 ml | 2.087 ml | 4.175 ml |
| 10 mM | 0.209 ml | 1.044 ml | 2.087 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.417 ml |
Last Update：2024-01-02 23:10:35
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride - Cell Experiment
Cell lines: A375 cells Concentrations: 0-20 μm incubation Time: 48 h method: A375 (CRL-1619) cells were cultured in DMEM medium containing 10% FBS. PRMT6 was cloned between the BamHI and coRI sites of the pcDNA4 HisMAX_A plasmid. Cells were seeded at a density of 200,000/well in 6-well plates. The following day his-tagged PRMT6 plasmid was transfected into the cells while they were treated with compound (compound concentration up to 20 μm) and the cell pellet was collected after 48 hours of treatment. For reference only.
Last Update：2023-08-16 21:32:38
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride - Animal Experiment
Animal Models: Sprague-Dawley rat Dosages: 1 mg/kg administration: intravenous for reference only
Last Update：2023-08-16 21:32:38
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Product Name: N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride Visit Supplier Webpage Request for quotation
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View History
N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride
酵母粉琼脂粉末培养基
Levocetirizine Amide (USP)
胆固醇-聚乙二醇-马来酰亚胺
4-溴-N-十二基-1-羟基-2-萘甲酰胺
酵母粉琼脂粉末培养基
Levocetirizine Amide (USP)
胆固醇-聚乙二醇-马来酰亚胺
4-溴-N-十二基-1-羟基-2-萘甲酰胺