Merck UK-59811 hydrochloride

UK-59811 hydrochloride

≥98% (HPLC)

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

Quality Level

100

assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Pfizer®

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

주관자

Pfizer

저장 온도

2-8°C

SMILES string

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

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.