2. Anti-infection
  3. Influenza Virus
  4. PB2-IN-2

PB2-IN-2 是一种口服有效的 PB2 抑制剂，其 RNP 抑制活性 (IC50) 为 0.2 nM，细胞水平复制抑制活性 (LRA EC50) 为 0.8 nM，细胞病变效应抑制活性 (CPE EC50) 为 0.1 nM。。PB2-IN-2 对一组甲型流感病毒株 (包括 H1N1pdm09、Lyon/1337/2007/H1N1、Tex12-Like/H3N2、PR/8/34/H1N1、WSN/1933/H1N1 及 rPR8(H1N1)/H7N9) 展现出纳摩尔水平的广谱抗病毒效力 (EC50 分别为 1.5、3.6、3.7、13.8、2.9 和 9.8 nM，且 CC50 值均大于 2 μM）。PB2-IN-2 拥有优异的代谢稳定性和药代动力学特征。PB2-IN-2 可用于抗流感研究。

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PB2-IN-2

PB2-IN-2 Chemical Structure

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PB2-IN-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PB2-IN-2 is an orally active PB2 inhibitor with RNA-dependent RNA Polymerase (RNP) IC50 = 0.2 nM, LRA (Ligand Receptor Assay) EC50 = 0.8 nM, Cytopathic Effect (CPE) EC50 = 0.1 nM. PB2-IN-2 exhibits broad-spectrum, nanomolar antiviral potency against a panel of influenza A strains (including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, rPR8(H1N1)/H7N9 with EC50 = 1.5, 3.6, 3.7, 13.8, 2.9 and 9.8 nM and all the CC50 values > 2 μM. PB2-IN-2 possesses an excellent pharmacokinetic profile and metabolic stability. PB2-IN-2 can be used for anti-influenza research[1].

体外研究
(In Vitro)

PB2-IN-2 (compound 3) 具有较低的亲脂性 (LogD 值为 1.27)[1]。
PB2-IN-2 在 A549 肺细胞中对一系列野生型和实验室适应的甲型流感病毒 (包括 H1N1pdm09、Lyon/1337/2007/H1N1、Tex12-Like/H3N2、PR/8/34/H1N1、WSN/1933/H1N1 以及 rPR8(H1N1)/H7N9 病毒株) 表现出卓越的抑制活性，其 EC50 分别为 1.5、3.6、3.7、13.8、2.9 和 9.8 nM，且所有 IC50 值均大于 2 μM，并且显示出良好的安全窗口[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PB2-IN-2 相关抗体:
体内研究
(In Vivo)

PB2-IN-2 (compound 3) 在小鼠体内表现出较高的游离血浆分数 (1.2%)[1]。
PB2-IN-2 (0.05-1 mg/kg，口服给药，每日两次，持续 5 天) 在甲型流感病毒小鼠感染模型中，具有低有效剂量、平缓的疗效-剂量关系及宽治疗窗等特征[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A/Puerto Rico/8/34 (3 × 105 TCID50, i.n.) induced-male BALB/c mice[1]
Dosage: 0.05, 0.1, 0.3, and 1 mg/kg
Administration: p.o., twice daily for 5 days
Result: Provided 100% protection at a minimum dose of 0.3 mg/kg.
Achieved full protection maintaining in vitro EC50 coverage for more than 18 h.
Lost peak body weight at 10% by day 7 and recovered by day 14 at 0.3 mg/kg.
分子量

412.39

Formula

C20H18F2N6O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PB2-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PB2-IN-2Influenza VirusPB2influenza A strainsinfluenzaInhibitorinhibitorinhibit

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