Aurintricarboxylic-acid-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAurintricarboxylic acidCat. No.: HY-122575CAS No.: 4431-00-9分式: CHO分量: 422.34作靶点: P2X Receptor; Influenza Virus; Topoisomerase作通路: Membrane Transporter/Ion Channel; Anti-infection; CellCycle/DNA Damage储存式: Powder -20C 3 years4C

2、2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (295.97 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3678 mL 11.8388 mL 23.6776 mL5 mM 0.4736 mL 2.3678 mL 4.7355 mL10 mM 0.2368 mL 1.1839 mL 2.3678 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，并请注意储备液的保存式和期限。体内实验 请根

3、据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.92 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.92

4、mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Aurintricarboxylic acid效的，- 亚甲-ATP 敏感选择性 P2X1Rs 和 P2X3Rs 变构拮抗剂，对 rP2X1R和 rP2X3R 作的 IC50 值分别为 8.6 nM 和 72.9 nM 1。Aurintricarboxylic acid种有效的抗流感剂，通过直接抑制神经氨酸酶 (neuraminidase) 作 2。Aurintricarboxylic acid 也拓扑异构酶 II

5、 和凋亡抑制剂3。Aurintricarboxylic acid选择性的 TWEAK-Fn14 信号通路抑制剂 4。Aurintricarboxylic acid 也种胱硫醚-裂解酶 (CSE) 抑制剂，其 IC50 值为 0.6 M 5。IC50 & Target Topoisomerase II rP2X1R rP2X3R Apoptosis8.6 nM (IC50) 72.9 nM (IC50)体外研究 Aurintricarboxylic acid strongly inhibits rP2X1Rs and rP2X3Rs with IC50 values of 8.6 nM and

6、72.9 nM,respectively, and more weakly inhibits P2X2/3Rs, P2X2Rs, P2X4Rs or P2X7Rs 1.Aurintricarboxylic acid inhibition of ATP-induced currents is concentration dependent 1.Aurintricarboxylic acid is a non-competitive antagonist of P2X3R 1.Aurintricarboxylic acid can inhibit the severe acute respirat

7、ory syndrome-associated coronavirus (SARS-CoV) and vaccinia virus 2.Aurintricarboxylic acid protects MDCK cells from infection with influenza A strains PR8, NY or N 2.Aurintricarboxylic acid inhibits replication of influenza A and B viruses 2.Aurintricarboxylic acid inhibits neuraminidase activities

8、 of influenza A and B viruses 2.Aurintricarboxylic acid inhibits TWEAK-Fn14-mediated NF-B activation 4.Aurintricarboxylic acid (10 M;0.5-2 hours) suppresses TWEAK-Fn14-mediated NF-B, Akt, and Srcphosphorylation in GBM cells 4.Aurintricarboxylic acid blocks TWEAK-stimulated Rac1 activation and TRAF2

9、recruitment to Fn14cytoplasmic domain in glioma cells 4.Aurintricarboxylic acid represses TWEAK-stimulated glioma cell migration and invasion without causing cellcytotoxicity 4.Western Blot Analysis 4Cell Line: T98G, A172, GBM44 glioma cellsConcentration: 10 MIncubation Time: 0.5 hour, 1 hour, 2 hou

10、rsResult: Abrogated TWEAK activation of downstream signals including phosphorylation of the NF-B family member p65, Akt, and Src in all three GBM cell lines.REFERENCES1. Obrecht AS, et al. Identification of aurintricarboxylic acid as a potent allosteric antagonist of P2X1 and P2X3 receptors.Neuropha

11、rmacology. 2019 Nov 1;158:107749.2. Hashem AM, et al. Aurintricarboxylic acid is a potent inhibitor of influenza A and B virus neuraminidases. PLoS One. 2009 Dec17;4(12):e8350.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE3. Benchokroun Y, et al. Aurintricarboxylic acid, a putative inhibitor of a

12、poptosis, is a potent inhibitor of DNA topoisomerase II in vitro and inChinese hamster fibrosarcoma cells. Biochem Pharmacol. 1995 Jan 31;49(3):305-13.4. Benchokroun Y, et al. Aurintricarboxylic acid, a putative inhibitor of apoptosis, is a potent inhibitor of DNA topoisomerase II in vitro and inChinese hamster fibrosarcoma cells. Biochem Pharmacol. 1995 Jan 31;49(3):305-13.5. Youtian Hu, et al. Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine -Lyase. J Med Chem. 2019 Feb14;62(3):1677-1683.McePdfHeigh