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(-)-[3R,4S]-Chromanol 293B
Chemical Name:N-[(3R,4S)-6-Cyano-3,4-dihydro-3-hydroxy-2,2-dimethyl-2
H-1-benzopyran-4-yl]-N-methylethanesulfonamide
Biological Activity:
Enantiomer that selectively inhibits the slow
component of delayed rectifier K+ current (IKs). Block is
use-dependent and 7-fold more potent than the (+)-(3S,4R) enantiomer (IC50
values are 1.36 and 9.6 μM
respectively). Has negligible inhibitory action at hERG channels (IC50
> 30 μM).
Yanget al (2000) Stereoselective
interactions of the enantiomers of chromanol 293B with human voltage-gated
potassium channels. J.Pharmacol.Exp.Ther. 294 955. Seebohmet al (2001) A kinetic study on the stereospecific inhibition of KCNQ1
and IKs by the chromanol 293B.
Br.J.Pharmacol. 134 1647. Lercheet al (2001)
Molecular impact of MinK on the enantiospecific block of IKs by chromanols. Br.J.Pharmacol. 131
1503.