芦平曲韦

芦平曲韦用途

Rupintrivirvr (AG7088),抗病毒药,是一种有效,选择性和不可逆的人类 rhinovirus (HRV) 3C protease 抑制剂。在 H1-Hela 和 MRC-5 细胞保护试验中,Rupintrivirvr 抑制48种不同HRV血清型的复制,平均 EC50 为 0.023 μM。Rupintrivirvr 具有免疫调节作用。

芦平曲韦名称

[ CAS 号 ]:
223537-30-2

[ 中文名 ]:
芦平曲韦

[ 英文名 ]:
Rupintrivir

[中文别名 ]:

[英文别名 ]:

ag7088
UNII-RGE5K1Q5QW
Ruprintrivir
Rupintrivir

芦平曲韦生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 炎症/免疫

[体外研究]

在H1-HeLa和MRC-5细胞保护试验中,Rupintrivirvr(AG7088)抑制所有HRV血清型(48/48)的复制,平均50%有效浓度(EC50)为0.023μM(范围0.003-0.081μM),平均EC90为0.082μM(范围0.082μM),0.018至0.261μM)以及相关的微微鸟氨酸病毒,包括柯萨奇病毒A21和B3、肠道病毒70和echovirus 11[1]。

[体内研究]

Rupintrivirvr(AG7088)降低HDM致敏小鼠离体肺切片(PCLS)中RV诱导的TH-2细胞因子IL-4的表达[2]。

[参考文献]

[1]. Patick AK, et al. In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease. Antimicrob Agents Chemother. 1999 Oct;43(10):2444-50.

[2]. Danov O, et al. Rupintrivir reduces RV-induced TH-2 cytokine IL-4 in precision-cut lung slices (PCLS) of HDM-sensitized mice ex vivo. Respir Res. 2019 Oct 22;20(1):228.

[3]. Dragovich PS, et al. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics. J Med Chem. 1999 Apr 8;42(7):1203-12.

芦平曲韦物理化学性质

[ 密度 ]:
1.213g/cm3

[ 沸点 ]:
866.7ºC at 760mmHg

[ 熔点 ]:
170-171°C

[ 分子式 ]:
C₃₁H₃₉FN₄O₇

[ 分子量 ]:
598.66200

[ 闪点 ]:
477.9ºC

[ 精确质量 ]:
598.28000

[ PSA ]:
156.70000

[ LogP ]:
3.93550

[ 蒸汽压 ]:
1.87E-30mmHg at 25°C

[ 折射率 ]:
1.537

[ 储存条件 ]:
室温

芦平曲韦安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

芦平曲韦文献

Crystal structures of enterovirus 71 3C protease complexed with rupintrivir reveal the roles of catalytically important residues.

J. Virol. 85(19) , 10021-30, (2011)

EV71 is the primary pathogenic cause of hand-foot-mouth disease (HFMD), but an effective antiviral drug currently is unavailable. Rupintrivir, an inhibitor against human rhinovirus (HRV), has potent a...

Conservation of amino acids in human rhinovirus 3C protease correlates with broad-spectrum antiviral activity of rupintrivir, a novel human rhinovirus 3C protease inhibitor.

Antimicrob. Agents Chemother. 49(2) , 619-26, (2005)

The picornavirus 3C protease is required for the majority of proteolytic cleavages that occur during the viral life cycle. Comparisons of published amino acid sequences from 6 human rhinoviruses (HRV)...

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