VX-787
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- CAS号:
- 1629869-44-8
- 英文名:
- Pimodivir
- 英文别名:
- VX-787;CS-2483;Pimodivir;VRT0928787;VRT 0928787;VRT-0928787;JNJ63623872;JNJ 63623872;JNJ-63623872;Pimodivir (VX-787)
- 中文名:
- VX-787
- 中文别名:
- 化合物PIMODIVIR
- CBNumber:
- CB03169595
- 分子式:
- C20H19F2N5O2
- 分子量:
- 399.39
- MOL File:
- 1629869-44-8.mol
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VX-787化学性质
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密度:
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1.501±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO, not in water:100.0(Max Conc. mg/mL);250.38(Max Conc. mM)
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形态:
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A solid
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酸度系数(pKa):
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4.32±0.40(Predicted)
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VX-787性质、用途与生产工艺
Pimodivir (VX-787) 是一种可口服的甲型流感病毒聚合酶抑制剂，通过抑制PB2亚基起作用。
Pimodivir rescues macrophages from virus-mediated death at non-cytotoxic concentrations 24 hpi. The EC
50
value for Pimodivir are 8 and 12 nM for A(H1N1) and A(H3N2) strains, respectively, whereas the CC
50
values are >1 μM, giving selectivity indexes (SI) > 125 and > 83 for A(H1N1) and A(H3N2) strains, respectively. Pimodivir significantly attenuates the transcription of viral M1 RNA in macrophages, which are infected with A(H1N1) or A(H3N2) strains for 8 h. Pimodivir inhibits the transcription of viral but not cellular genes. Pimodivir allows some activation of IAV-mediated expression of several cellular genes, which are involved in tryptophan and nucleotide metabolism. Pimodivir possesses excellent anti-IAV but not immuno/metabolo-modulating effect. Pimodivir (VX-787) is very potent against influenza A strains, including pandemic 2009 H1N1 and avian H5N1. Pimodivir (VX-787) shows potent activity against all influenza A virus strains tested, with an EC
50
range of 0.13 to 3.2 nM. Pimodivir-selected PB2 variant viruses maintain susceptibility to neuraminidase inhibitors in vitro.
Pimodivir (2, 6, and 20 mg/kg/day, p.o.) and GS 4071 (20 mg/kg/day) completely prevent death in the H1N1pdm virus infection in mice. Pimodivir (20 mg/kg/day) is more effective than GS 4071 (20 mg/kg/day) in improving body weight and reducing the severity of lung infection. Moreover, Pimodivir (VX-787) shows 100% survival in a +48 h delay to treatment mouse influenza model at 10, 3 and 1 mpk (BID × 10 days) whereas the SOC, GS 4071, provide no survival benefit in this model at 10 mpk. Pimodivir (VX-787; 1, 3, or 10 mg/kg, bid) provided complete survival, with a dose-dependent reduction in BW loss of the mice.
VX-787
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-12353A | VX-787
Pimodivir | 1629869-44-8 | 5mg | 900元 |
| 2024/04/30 | HY-12353A | VX-787
Pimodivir | 1629869-44-8 | 10mg | 1500元 |
1629869-44-8, VX-787 相关搜索:
- 库存
- 化合物PIMODIVIR
- 1629869-44-8
- JNJ-63623872
- JNJ63623872
- JNJ 63623872
- Influenza Virus,Inhibitor,inhibit,VX787,Pimodivir,VX 787
- VRT 0928787
- CS-2483
- (2S,3S)-3-[[5-Fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]bicyclo[2.2.2]octane-2-carboxylic acid
- Bicyclo[2.2.2]octane-2-carboxylic acid, 3-[[5-fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-4-pyrimidinyl]amino]-, (2S,3S)-
- VX-787 (Pimodivir)
- VX-787; VX 787; VX787; JNJ-872; JNJ 872; JNJ872; VRT-0928787; VRT 0928787; VRT0928787;PIMODIVIR
- VRT-0928787
- VRT0928787
- VX-787
- Pimodivir (VX-787)
- Pimodivir