PZ0353
UK-59811 hydrochloride
≥98% (HPLC)
别名:
4-(2-Bromophenyl)-2-[[2-(dimethylamino)ethoxy]methyl]-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester hydrochloride, UK59811 hydrochloride
InChI
1S/C22H29BrN2O5/c1-6-30-22(27)20-17(13-29-12-11-25(3)4)24-14(2)18(21(26)28-5)19(20)15-9-7-8-10-16(15)23/h7-10,19,24H,6,11-13H2,1-5H3
InChI key
XCBGSNNUPRHJGR-UHFFFAOYSA-N
SMILES string
CCOC(C1=C(COCCN(C)C)NC(C)=C(C(OC)=O)C1C2=C(Br)C=CC=C2)=O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
法规信息
新产品
此项目有
Lin Tang et al.
Nature, 537(7618), 117-121 (2016-08-25)
Ca2+ antagonist drugs are widely used in therapy of cardiovascular disorders. Three chemical classes of drugs bind to three separate, but allosterically interacting, receptor sites on CaV1.2 channels, the most prominent voltage-gated Ca2+ (CaV) channel type in myocytes in cardiac
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