VU 0240551
A KCC2 cotransporter inhibitor
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包装价格促销价数量
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5mg￥1350.001080.00- +
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10mg￥1750.001400.00- +
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50mg￥7350.005880.00- +
- 货号: ajce60096
- CAS: 893990-34-6
- 别名: N-(4-甲基-2-噻唑基)-2-[(6-苯基-3-哒嗪基)硫基]-乙酰胺
- 分子式: C16H14N4OS2
- 分子量: 342.44
- 纯度: ＞98%
- 溶解度: DMSO: ≥ 50 mg/mL (146.01 mM); Water: < 0.1 mg/mL (insoluble)
- 储存: Store at -20°C
- 库存: 现货
Background
VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).1 It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 ?M) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 ?M. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 ?M.
1.Delpire, E., Days, E., Lewis, L.M., et al.Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2Proc. Natl. Acad. Sci. USA106(13)5383-5388(2009)
