Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC 50 s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC 50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC 50 of 0.47 μM.
性状
Solid
IC50 & Target[1][2]
Topoisomerase II rP2X1R 8.6 nM (IC50)
体外研究(In Vitro)
Aurintricarboxylic acid weakly inhibits P2X2/3Rs, P2X2Rs, P2X4Rs or P2X7Rs.Aurintricarboxylic acid inhibits ATP-induced currents in a concentration dependent manner.Aurintricarboxylic acid can inhibit the severe acute respiratory syndrome-associated coronavirus (SARS-CoV) and vaccinia virus.Aurintricarboxylic acid inhibits replication of influenza A and B viruses by inhibition of neuraminidase activities.Aurintricarboxylic acid inhibits TWEAK-Fn14-mediated NF-κB activation.Aurintricarboxylic acid (10 μM; 0.5-2 hours) suppresses TWEAK-Fn14-mediated NF-κB, Akt, and Src phosphorylation in GBM cells.Aurintricarboxylic acid represses TWEAK-stimulated glioma cell migration and invasion without causing cell cytotoxicity.Aurintricarboxylic acid (Compound 8) cannot regulate loading of endogenous let-7 onto AGO2 inside cultured cells, whereas can inhib
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
参考文献
[1]. Obrecht AS, et al. Identification of aurintricarboxylic acid as a potent allosteric antagonist of P2X1 and P2X3 receptors. Neuropharmacology. 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 Dec 17;4(12):e8350.
溶解度数据
In Vitro: DMSO : 125 mg/mL (295.97 mM; Need ultrasonic)H2O : < 0.1 mg/mL (ultrasonic) (insoluble)配制储备液