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CAS No.: 265646-85-3

Emidurdar Catalog No. CSN33111

Synonyms: NS3728;SCO‐101

Endovion is a blocker of both VRAC and CaCC with IC50 value around 400nM for blocking swelling-activated anion currents in HEK293 cells.

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400-920-2911

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技术信息

生物活性

描述The Volume-Regulated Anion Channel (VRAC) is activated by cell swelling and plays a key role in cell volume regulation. VRAC is ubiquitously expressed in vertebrate cells and also implicated in many other physiological and cellular processes including fluid secretion, glutamate release, membrane potential regulation, cell proliferation, migration, and apoptosis^[1]. In addition to its role in cell volume homeostasis, VRAC has been implicated in numerous other physiological and pathophysiological processes, including cancer, ischemic brain edema, cell motility, proliferation, angiogenesis, programmed cell death, and excitotoxic glutamate release^[2]. VRAC is formed by hetero-hexamers of members of the LRRC8 protein family, which consists of five members, LRRC8A-E. LRRC8A is an essential subunit for physiological functionality of VRAC. Its obligate heteromerization with at least one of its paralogues, LRRC8B-E, determines the biophysical properties of VRAC^[3]. Anoctamin (Ano)-1, a calcium-activated chloride channel, can regulate cell proliferation and cell cycle in multiple cell types^[4]. Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor. Endovion (10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines^[5]. Endovion (10-100 μM) reduces TNFα-induced apoptosis and increases p53-protein level as well as downstream signaling, e.g., expression of p21Waf1/Cip1, Bax, Noxa, MDM2, and activation of Caspase-9/-3 in Cisplatin-sensitive cells^[6].
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
- 2.0195 mL
- 10.0974 mL
- 20.1948 mL
- 5 mM
- 0.4039 mL
- 2.0195 mL
- 4.0390 mL
- 10 mM
- 0.2019 mL
- 1.0097 mL
- 2.0195 mL

技术信息

CAS号	265646-85-3	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	C16H9BrF6N6O	运输	蓝冰
分子量	495.18	别名	NS3728;SCO‐101

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