ML365 |
| رقم الكتالوجGC36629 |
ML365 هو مثبط انتقائي لقناة KCNK3 / TASK1 لقناة البوتاسيوم ذات المسام ، مع IC50 من 4 نانومتر
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Cas No.: 947914-18-3
Sample solution is provided at 25 µL, 10mM.
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ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).IC50 value: 4 nM/16 nM(thallium influx fluorescent assay/automated electrophysiology assay) [1]Target: KCNK3 blockerML365 possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.
[1]. Zou B, et al. ML365: Development of Bis-Amides as Selective Inhibitors of the KCNK3/TASK1 Two Pore Potassium Channel. Probe Reports from the NIH Molecular Libraries Program [Internet].
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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