巴洛沙韦 T14495

Product Introduction
Bioactivity


英文名: Baloxavir

描述: Baloxavir (S-033447) 是衍生自前药 Baloxavir marboxil，是流感病毒聚合酶 PA 亚基的一流帽依赖性核酸内切酶抑制剂。它抑制病毒 RNA 的转录和复制，具有强大的抗病毒活性。

体外活性: Baloxavir (BXA) inhibits viral RNA transcription via selective inhibition of cap-dependent endonuclease (CEN) activity in enzymatic assays, and inhibits viral replication in infected cells without cytotoxicity in cytopathic effect assays, and it also inhibits cap-dependent endonuclease (CEN) and CEN/RdRp activities with IC50 values of 2.5 nM and 1.6 nM, respectively, while low potency (IC50 >40 nM) is observed against RdRp activity[2]. The median EC50 values at baseline for Baloxavir (BXA) are 17.96 nM for A/H1N1pdm, 4.48 nM for A/H3N2, and 18.67 nM for type B virus[1]. Baloxavir shows high potency against influenza A and B viruses with mean EC90 of 0.46 - 0.98 nM and 2.2-3.4 nM, respectively[2] and it also shows broad potency against various subtypes of influenza A viruses (H1N2, H5N1, H5N2, H5N6, H7N9 and H9N2). Additionally, serial passages of the viruses in the presence of Baloxavir result in isolation of PA/I38T variants with reduced BXA susceptibility[2]. Baloxavir (BXA) has a high inhibitory potency against CEN activity of the tested viral ribonucleoprotein complexes (vRNPs) from influenza A and B viruses with mean IC50 values of 1.4-3.1 nM and 4.5-8.9 nM, respectively, indicating that Baloxavir has broad spectrum activities.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (93.07 mM)


关键字: inhibit | CEN | BXA | cap-dependent | dolutegravir | S033447 | influenza | Baloxavir | RNA | replication | S 033447 | endonuclease | Inhibitor | transcription

相关产品: Tulobuterol hydrochloride | Lapachol | Chelidonine | Oplodiol | Rupestonic acid | XSJ2-46 | Aurintricarboxylic acid | RdRP-IN-5 | Neuraminidase-IN-1 | Emricasan

相关库: Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Anti-Viral Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library

巴洛沙韦 T14495信息由TargetMol中国为您提供，如您想了解更多关于巴洛沙韦 T14495报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途