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UK-59811 hydrochloride,≥98% (HPLC)

别名:UK59811 hydrochloride, 4-(2-Bromophenyl)-2-[[2-(dimethylamino)ethoxy]methyl]-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester hydrochloride

Empirical Formula (Hill Notation): C22H29BrN2O5 · HCl 分子量: 517.84 NACRES: NA.77
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): PZ0353
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$354.21

说明

生化/生理作用

UK-59811 is a 1,4-dihydropyridine calcium channel blocker. It has been used in a crystallographic and functional analysis of drug binding to the bacterial homotetrameric model voltage-gated calcium channel CaVAb, comparing 1,4-dihydropyridine binding to phenylalkylamine binding. UK-59811 inhibited CaVAb with an IC50 value of 194 nM, binding at the outer, lipid-facing surface of the pore at the interface between two CaVAb subunits, while at concentrations above 1 μM, it also bound in the pore. It was contrasted with phenylalkylamine Br-verapamil which binds on the intracellular side of the selectivity filter in the central cavity of the pore, physically blocking the pore.
 
UK-59811 是一种 1,4-二氢吡啶钙通道阻滞剂。 它已用于药物与细菌同源四聚体模型电压门控钙通道 CaVAb 的晶体学和功能分析,比较 1,4-二氢吡啶结合与苯烷基胺结合。 UK-59811 以 194 nM 的 IC50 值抑制 CaVAb,结合在两个 CaVAb 亚基之间界面处的孔外、面向脂质的表面,而当浓度高于 1 μM 时,它也结合在孔中。 它与苯烷基胺 Br-维拉帕米形成对比,后者结合在孔中央腔的选择性过滤器的细胞内侧,物理堵塞孔。
 

法律信息

Sold for research purposes under agreement from Pfizer Inc.
Pfizer is a registered trademark of Pfizer, Inc.
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

mfr. no.

Pfizer®

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

创始人

Pfizer

储存温度

2-8°C

SMILES string

CCOC(C1=C(COCCN(C)C)NC(C)=C(C(OC)=O)C1C2=C(Br)C=CC=C2)=O

 

安全信息

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 33 | 欧洲Eur. ≥ 27 | 東京Tokyo ≥ 9 | 香港与北京 ≥ 16