Aurintricarboxylic acid 是高效的，αβ-亚甲基-ATP 敏感选择性P2X1Rs和P2X3Rs变构拮抗剂，对 rP2X1R 和 rP2X3R 作用的IC50值分别为 8.6 nM 和 72.9 nM。Aurintricarboxylic acid 是一种有效的抗流感剂，通过直接抑制神经氨酸酶 (neuraminidase) 作用。Aurintricarboxylic acid 也是拓扑异构酶 II和凋亡抑制剂。Aurintricarboxylic acid 是选择性的TWEAK-Fn14信号通路抑制剂。Aurintricarboxylic acid 也是一种胱硫醚-γ-裂解酶 (CSE) 抑制剂，其IC50值为 0.6 μM。Aurintricarboxylic acid 是能够调节 miRNA 功能的miRNA调节剂。
| 生物活性 | Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitiveP2X1RsandP2X3Rs, withIC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively[1]. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting theneuraminidase[2]. Aurintricarboxylic acid is an inhibitor oftopoisomeraseIIandapoptosis[3]. Aurintricarboxylic acid is a selective inhibitor of theTWEAK-Fn14signaling pathway[4]. Aurintricarboxylic acid also acts as acystathionine-lyase (CSE)inhibitor with anIC50of 0.6 μM[5]. Aurintricarboxylic acid is a modifier ofmiRNAsthat regulate miRNA function, with anIC50of 0.47 μM[6]. |
| IC50& Target[1][3][6] | Topoisomerase II | rP2X1R 8.6 nM (IC50) | rP2X3R 72.9 nM (IC50) | Apoptosis | miRNA 0.47 μM (IC50) |
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体外研究
(In Vitro) | Aurintricarboxylic acid weakly inhibits P2X2/3Rs, P2X2Rs, P2X4Rs or P2X7Rs[1].
Aurintricarboxylic acid inhibits ATP-induced currents in a concentration dependent manner[1].
Aurintricarboxylic acid can inhibit the severe acute respiratory syndrome-associated coronavirus (SARS-CoV) and vaccinia virus[2].
Aurintricarboxylic acid inhibits replication of influenza A and B viruses by inhibition of neuraminidase activities[2].
Aurintricarboxylic acid inhibits TWEAK-Fn14-mediated NF-κB activation[4].
Aurintricarboxylic acid (10 μM; 0.5-2 hours) suppresses TWEAK-Fn14-mediated NF-κB, Akt, and Src phosphorylation in GBM cells[4].
Aurintricarboxylic acid represses TWEAK-stimulated glioma cell migration and invasion without causing cell cytotoxicity[4].
Aurintricarboxylic acid (Compound 8) cannot regulate loading of endogenous let-7 onto AGO2 inside cultured cells, whereas can inhibit RISC loading of exogenous siRNA[6].
Western Blot Analysis[4] | Cell Line: | T98G, A172, GBM44 glioma cells | | Concentration: | 10 μM | | Incubation Time: | 0.5 hour, 1 hour, 2 hours | | Result: | Abrogated TWEAK activation of downstream signals including phosphorylation of the NF-κB family member p65, Akt, and Src in all three GBM cell lines. |
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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(295.97 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 2.3678 mL | 11.8388 mL | 23.6776 mL | | 5 mM | 0.4736 mL | 2.3678 mL | 4.7355 mL | | 10 mM | 0.2368 mL | 1.1839 mL | 2.3678 mL |
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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
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此方案可获得 ≥ 2.08 mg/mL (4.92 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% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.92 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.92 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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