Endovion (NS3728) 是一种阴离子通道抑制剂 (如氯离子通道),也是特异性的VRAC/VSOAC阻断剂。Endovion (NS3728) 还是一种ANO1抑制剂。
生物活性 | Endovion (NS3728) is a pharmacologicalanion channel inhibitor (like chloride channel)and the specificVRAC/VSOACblocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor[1][2]. |
IC50& Target | Chloride channel, VRAC/VSOAC[1]. ANO1[2]. |
体外研究 (In Vitro) | Endovion (NS3728, 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[1]. Endovion (NS3728, 10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines[2].
Western Blot Analysis[1] Cell Line: | Wild-type, resistant, and transiently transfected A2780 cells. | Concentration: | 10-100 μM. | Incubation Time: | 18 or 4.5 h. | Result: | Reduced the maximal taurine rate constant more than 90% compared with the untreated control cells. Resulted in an increased LRRC8A protein expression. Significantly reduceed p53 andp21Waf1/Cip1protein level in A2780WT cells.
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Cell Proliferation Assay[2] Cell Line: | Capan-1, AsPC-1, BxPC-3 and H6c7 cell lines. | Concentration: | 10 μM. | Incubation Time: | 24 h. | Result: | Resulted in the most pronounced inhibition in all cell lines with 77 ± 26 % in Capan-1, 67 ± 9 % in AsPC-1, and 54 ± 8 % in BxPC-3 cells at +67 mV. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(252.43 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 1 mM | 2.0195 mL | 10.0973 mL | 20.1947 mL | 5 mM | 0.4039 mL | 2.0195 mL | 4.0389 mL | 10 mM | 0.2019 mL | 1.0097 mL | 2.0195 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.20 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.20 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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