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首页 / 抑制剂/激动剂 / 抗感染 / 巨细胞病毒 / Maribavir/马立巴韦

Maribavir/马立巴韦 {[allProObj[0].p_purity_real_show]}

货号：A851897 同义名： GW257406X; 1263W94

Maribavir是一种有效的野生型pUL97催化的组蛋白磷酸化抑制剂，IC50为3 nM。它对HCMV和Epstein-Barr病毒（EBV）具有强效的抗病毒活性。

Maribavir/马立巴韦 化学结构 CAS号：176161-24-3
Maribavir/马立巴韦 化学结构
CAS号：176161-24-3
Maribavir/马立巴韦 3D分子结构
CAS号：176161-24-3
Maribavir/马立巴韦 化学结构 CAS号：176161-24-3
Maribavir/马立巴韦 3D分子结构 CAS号：176161-24-3
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Maribavir/马立巴韦 纯度/质量文件 产品仅供科研

货号：A851897 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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Maribavir/马立巴韦 生物活性

描述 Maribavir effectively inhibits the autophosphorylation of both wild-type and major Ganciclovir (GCV) resistant UL97 mutants, with an average IC50 of 35 nM. The M460I mutation exhibits increased sensitivity to Maribavir, having an IC50 of 4.8 nM, while the Maribavir-resistant UL97 mutant L397R shows reduced kinase activity to about 10% of the wild type. Enzyme kinetics reveal Maribavir acts as a competitive inhibitor of ATP with a Ki of 10 nM[1]. Additionally, Maribavir suppresses viral replication dose-dependently with an IC50 of 0.12±0.01 μM in multicycle DNA hybridization assays, and strongly inhibits the pUL97 protein kinase at a 50% inhibition concentration of 3 nM[2].
体外研究

Maribavir effectively inhibits the autophosphorylation of both wild-type and major Ganciclovir (GCV) resistant UL97 mutants, with an average IC50 of 35 nM. The M460I mutation exhibits increased sensitivity to Maribavir, having an IC50 of 4.8 nM, while the Maribavir-resistant UL97 mutant L397R shows reduced kinase activity to about 10% of the wild type. Enzyme kinetics reveal Maribavir acts as a competitive inhibitor of ATP with a Ki of 10 nM[1].

Additionally, Maribavir suppresses viral replication dose-dependently with an IC50 of 0.12±0.01 μM in multicycle DNA hybridization assays, and strongly inhibits the pUL97 protein kinase at a 50% inhibition concentration of 3 nM[2].

Maribavir/马立巴韦 细胞实验

Cell Line
Concentration Treated Time Description References
Akata cells 20 µM 24 hours MBV inhibits phosphorylation of EBV early antigen EA-D J Virol. 2009 Dec;83(23):12108-17.
Akata cells 20 µM 24 hours MBV almost completely inhibited the appearance of the 54-kDa and 52-kDa EA-D products and also reduced the level of 49-kDa EA-D J Virol. 2009 Dec;83(23):12108-17.
293 cells 20 µM 48 hours MBV inhibits EBV transcription and replication by inhibiting BGLF4 protein kinase activity J Virol. 2013 May;87(9):5311-5.
Human foreskin fibroblasts (HFF) 10 µM 5 to 6 days To evaluate the effect of MBV on GCV antiviral activity, results showed MBV increased GCV EC50 by 13-fold Antimicrob Agents Chemother. 2006 Oct;50(10):3470-2.
Human embryonic lung (HEL) fibroblasts 0.32 µM 5 to 6 days To evaluate the effect of MBV on GCV antiviral activity, results showed MBV increased GCV EC50 by ninefold Antimicrob Agents Chemother. 2006 Oct;50(10):3470-2.
Human foreskin fibroblast (HFF) 0.5-25 µM 5-20 passages Selection of UL97 and UL27 mutations, discovery of new UL97 mutation L337M and UL27 mutations D534Y, R448P Antiviral Res. 2012 Aug;95(2):88-92.
ARPEp cells 48.0 µM 6 days Evaluate the inhibitory effect of Maribavir on L397R mutant CMV, EC50 was 48.0 μM Antiviral Res. 2024 Feb;222:105792.
ARPEp cells 0.118 µM 6 days Evaluate the inhibitory effect of Maribavir on wild-type CMV, EC50 was 0.118 μM Antiviral Res. 2024 Feb;222:105792.
MRC-5 fibroblasts 40 µM 72 hours Evaluate the inhibitory effect of MBV on hCMV DNA synthesis, results showed MBV alone reduced viral DNA levels by an average of 95% Antiviral Res. 2013 Nov;100(2):321-7.
U373 cells 40 µM 72 hours Evaluate the inhibitory effect of MBV on hCMV DNA synthesis, results showed MBV alone reduced viral DNA levels by an average of 40% Antiviral Res. 2013 Nov;100(2):321-7.
Human embryonic lung fibroblasts 0.1-10 µM weekly passage To evaluate the antiviral activity of Maribavir against CMV and the emergence of resistance mutations Antimicrob Agents Chemother. 2009 Jan;53(1):81-5.

Maribavir/马立巴韦 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00002373 Cytomegalovirus Infections ... 展开 >> HIV Infections 收起 << Phase 1 Completed - United States, California ... 展开 >> Univ of California/ San Francisco / Dept of Medicine San Francisco, California, United States, 94110 Dr Jacob Lalezari San Francisco, California, United States, 94115 收起 <<
NCT00411645 Cytomegalovirus Infections Phase 3 Completed - -
NCT00497796 Cytomegalovirus Infections Phase 3 Completed - -

Maribavir/马立巴韦 参考文献

[1]Shannon-Lowe CD, et al. The effects of Maribavir on the autophosphorylation of ganciclovir resistant mutants of the cytomegalovirus UL97 protein. Herpesviridae. 2010 Dec 7;1(1):4.

[2]Biron KK, et al. Potent and selective inhibition of human cytomegalovirus replication by 1263W94, a benzimidazole L-riboside with a unique mode of action. Antimicrob Agents Chemother. 2002 Aug;46(8):2365-72.

Maribavir/马立巴韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.29mL

2.66mL

1.33mL

26.58mL

5.32mL

2.66mL

Maribavir/马立巴韦 技术信息

CAS号176161-24-3
分子式C15H19Cl2N3O4
分子量 376.24
SMILES Code CC(C)NC1=NC2=C(C=C(Cl)C(Cl)=C2)N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O
MDL No. MFCD00945570
别名 GW257406X; 1263W94; VP-41263; SHP-620; GW-1263; BW1263W94
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 190 mg/mL(505 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
方案 四
方案 五

Tags: Maribavir | 176161-24-3 | 1263W94 | BW1263W94 | GW257406X | Anti-infection | EBV | CMV | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Maribavir/马立巴韦 纯度/质量文件 | Maribavir/马立巴韦 生物活性 | Maribavir/马立巴韦 临床数据 | Maribavir/马立巴韦 参考文献 | Maribavir/马立巴韦 实验方案 | Maribavir/马立巴韦 技术信息

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