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CAS No.: 947914-18-3

ML365 Catalog No. CSN18626

Synonyms: ML365

ML365 is a selective small molecule inhibitor of TASK1 (KCNK3) with IC50 of 4 nM (thallium influx fluorescent assay) and 16 nM (automated electrophysiology assay).

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技术信息

生物活性

描述ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. 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). ML365 does not exhibit acute toxicity in cell-based assays at concentrations up to 30 μM^[3]. ML 365 also evoked a rapid increase in type-1 cell [Ca2+ ]i^[4]. ML365 was the most potent TWIK2 channel blocker with an IC50 value of 4.07 ± 1.5 μM. Furthermore, ML365 selectively inhibited TWIK2 without affecting TWIK1 or THIK1 channels. ML365 (1, 5 μM) concentration-dependently inhibited ATP-induced NLRP3 inflammasome activation in LPS-primed murine BMDMs, whereas it did not affect nigericin-induced NLRP3, or non-canonical, AIM2 and NLRC4 inflammasomes activation. Knockdown of TWIK2 significantly impaired the inhibitory effect of ML365 on ATP-induced NLRP3 inflammasome activation. Moreover, we demonstrated that pre-administration of ML365 (1, 10, 25 mg/kg, ip) dose-dependently ameliorated LPS-induced endotoxic shock in mice^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7747 mL
- 13.8733 mL
- 27.7465 mL
- 5 mM
- 0.5549 mL
- 2.7747 mL
- 5.5493 mL
- 10 mM
- 0.2775 mL
- 1.3873 mL
- 2.7747 mL

技术信息

CAS号

947914-18-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H20N2O3

运输

蓝冰

分子量

360.41

别名

ML365

溶解度

DMSO	72.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	18.0 mg/mL (49.9 mM)

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