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ML252
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ML252
Кол-во:
Фасовка:
Цена по запросу
Товар оформляется под заказ
Кол-во:
Фасовка:
Цена по запросу
Товар оформляется под заказ
Description_x000D_
Packaging_x000D_
5, 25 mg in glass bottle_x000D_
Biochem/physiol Actions_x000D_
ML252 is a potent, brain penetrant potassium channel Kv7.2 (KCNQ2) inhibitor with an IC50 of 69 nM. ML252 is only slightly selective over KCNQ3 and KCNQ4 but is over 40-fold selective for KCNQ2 vs KCNQ1, unlike other KCNQ inbhibitors currently used. ML252 was also selective vs. >68 tested GPCRs, ion channels, and transporters. Potassium channel Kv7.2 has become a new target for Alzheimer′s Disease drug research because inhibiting it enhances acetylcholine release. SAR studies showed a small structural change from ethyl group to hydrogen resulted in a functional shift from antagonist to agonist activity (37, EC50 of 170 nM), suggesting an interaction at a critical site for controlling KCNQ2 channel gating.
Related Categories
Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Ion Channels, M, Monovalent Ion Channels, Potassium Channel Modulators, Voltage-gated Ion ChannelsMore... Quality Level
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