产品说明书

Emidurdar

Print
Chemical Structure| 265646-85-3 同义名 : Endovion;NS 3728;SCO‐101;SCO-101
CAS号 : 265646-85-3
货号 : A1157109
分子式 : C16H9BrF6N6O
纯度 : 97%
分子量 : 495.177
MDL号 : MFCD28147607
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(242.34 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.10mL

2.02mL

1.01mL

20.19mL

4.04mL

2.02mL
参考文献

[1]James Osei-Owusu,et al. Molecular Biology and Physiology of Volume-Regulated Anion Channel (VRAC). Curr Top Membr.2018;81:177-203.

[2]Stine F Pedersen,et al. Biophysics and Physiology of the Volume-Regulated Anion Channel (VRAC)/Volume-Sensitive Outwardly Rectifying Anion Channel (VSOR). Pflugers Arch.2016 Mar;468(3):371-83.

[3]Sumaira Pervaiz,et al. Absolute Protein Amounts and Relative Abundance of Volume-regulated Anion Channel (VRAC) LRRC8 Subunits in Cells and Tissues Revealed by Quantitative Immunoblotting. Int J Mol Sci. 2019 Nov 23;20(23):5879.

[4] Ayed M Allawzi,et al. Activation of Anoctamin-1 Limits Pulmonary Endothelial Cell Proliferation via p38-Mitogen-activated Protein Kinase-Dependent Apoptosis. Am J Respir Cell Mol Biol. 2018 May;58(5):658-667.

[5]Sauter DR, et al. ANO1 (TMEM16A) in pancreatic ductal adenocarcinoma (PDAC). Pflugers Arch. 2015 Jul;467(7):1495-1508.

[6]Sørensen BH, et al. Downregulation of LRRC8A protects human ovarian and alveolar carcinoma cells against CDDP-induced expression of p53, MDM2, p21Waf1/Cip1, and Caspase-9/-3 activation. Am J Physiol Cell Physiol. 2016 Jun 1;310(11):C857-73.