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Merck
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Key Documents

SML0723

Sigma-Aldrich

ML252

≥98% (HPLC)

别名:

(S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide

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About This Item

经验公式(希尔记法):
C20H24N2O
分子量:
308.42
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

, light to dark purple

溶解度

DMSO: 25 mg/mL, clear

儲存溫度

2-8°C

生化/生理作用

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.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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