購物車 
-
法匹拉韋
- names：
Favipiravir
- CAS號：
259793-96-9
MDL Number： MFCD16879084 - MF(分子式)： C5H4FN3O2 MW(分子量)： 157.0287545
- EINECS: Reaxys Number:
- Pubchem ID:492405 Brand:BIOFOUNT
法匹拉韋（Favipiravir,259793-96-9）是一種吡嗪甲酰胺衍生物，F(xiàn)avipiravir具有抗RNA病毒活性。Favipiravir 通過宿主酶轉(zhuǎn)化為呋喃三磷酸核糖酯衍生物，可以選擇性地抑制流感病毒RNA依賴的RNA聚合酶。
| 貨品編碼 | 規(guī)格 | 純度 | 價格 (￥) | 現(xiàn)價(￥) | 特價(￥) | 庫存描述 | 數(shù)量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| HCQ000001-1g | 1g | 98% | ￥ 1200.00 | ￥ 1200.00 | instock | ￥ 0.00 | ||
| HCQ000001-100mg | 100mg | 98% | ￥ 580.00 | ￥ 580.00 | instock | ￥ 0.00 |
| 中文別名 | 法維拉韋;法匹沙韋;法匹拉韋（CAS:259793-96-9,MSDS,應(yīng)用,溶解度,）,法匹拉韋雜質(zhì) |
| 英文別名 | Favipiravir,259793-96-9,Favipiravir (T-705),T 705,T-705,T705 |
| CAS號 | 259793-96-9 |
| Inchi | InChI=1S/C22H25BrN2O3S/c1-5-28-22(27)20-18(13-29-14-9-7-6-8-10-14)25(4)17-11-16(23)21(26)15(19(17)20)12-24(2)3/h6-11,26H,5,12-13H2,1-4H3 |
| InchiKey | KCFYEAOKVJSACF-UHFFFAOYSA-N |
| 分子式 Formula | C5H4FN3O2 |
| 分子量 Molecular Weight | 157.0287545 |
| 溶解度Solubility | |
| 性狀 | 固體粉末 |
| 儲藏條件 Storage conditions | Store at room temperature |
法匹拉韋（CAS:259793-96-9,英文名:favipiravir）Protocol:
| 法匹拉韋細(xì)胞實驗 | |
|---|---|
| Cell lines | MDCK cells, Vero cells, HEL cells, A549 cells, HeLa cells, and HEp-2 cells |
| Preparation method | The cytotoxicity of T-705 is evaluated by an assay with XTT. XTT is converted to aqueous formazan by an enzyme in MDCK cells, Vero cells, HEL cells, A549 cells, HeLa cells, and HEp-2 cells. The compounds are diluted to the appropriate concentrations (volume, 100 μl) with test medium (EMEM containing 10% FCS) in 96-well culture plates in which each well contains a concentration of 2 × 103 cells/100 μL. The test plates are incubated for 3 days at 37°C in 100% humidity and 5% CO2. After 3 days, 50 μl of the XTT reagent (1 mg/ml in FCS-free EMEM containing 5 mM phenazine methosulfate) is added, and the reaction product is assayed by measurement of the absorbance at 450 nm with a microplate reader. Cytotoxicity is expressed as the 50% cell-inhibitory concentration (CC50). |
| Concentrations | 1000 μg/mL |
| Incubation time | 3 d |
|
法匹拉韋動物實驗
|
|
|---|---|
| Animal models | Mice infected with influenza virus A/PR/8/34 |
| Formulation | 0.5% methylcellulose |
| Dosages | 200 mg/kg/day |
| Administration | p.o. |
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Tags:法匹拉韋 試劑,法匹拉韋 抑制劑,法匹拉韋 衍生物,法匹拉韋 磷酸鹽衍生物,法匹拉韋 雜質(zhì),法匹拉韋 中間體,法匹拉韋 公司,法匹拉韋 購買;法匹拉韋 供應(yīng)商,
| 產(chǎn)品說明 | 法匹拉韋（259793-96-9,favipiravir）5-羥基-法匹拉韋,法匹拉韋一磷酸,法匹拉韋二磷酸,法匹拉韋三磷酸均為有效的病毒抑制劑 |
| Introduction | Favipiravir（259793-96-9）Favipiraviris triphosphate are initially approved for therapeutic use in resistant cases of influenza.7,9 The antiviral targets RNA-dependent RNA polymerase (RdRp) enzymes. |
| Application1 | 潛在冠狀病毒抑制劑Experimental Unapproved Treatments for COVID-19,may be an alternative option for influenza strains that are resistant to neuramidase inhibitors.9,19 |
| Application2 | 法匹拉韋在人體內(nèi)通過與糖作用生成“SCHEMBL7215591”，之后在結(jié)合磷酸鹽生成法匹拉韋三磷酸形式產(chǎn)物，最終對病毒產(chǎn)生作用。 |
| Application3 | Favipiravir has been investigated for the treatment of life-threatening pathogens such as Ebola virus, Lassa virus, and now COVID-19.10,14,15 |
法匹拉韋（CAS:259793-96-9,英文名:favipiravir）不僅可以抑制甲型和乙型流感病毒的復(fù)制，而且該藥在禽流感的治療中也有不錯的療效，并且可能是對神經(jīng)酰胺酶抑制劑有抗藥性的流感菌株的替代選擇。可以作為治療威脅生命的病原體，例如埃博拉病毒，拉沙病毒和現(xiàn)在的COVID-19
Favipiravir作為前藥起作用，并在細(xì)胞內(nèi)進(jìn)行核糖基化和磷酸化，成為活性的Favipiravir-RTP。Favipiravir-RTP結(jié)合并抑制RNA依賴性RNA聚合酶（RdRp），最終可以阻止病毒轉(zhuǎn)錄和復(fù)制。
與現(xiàn)有的流感抗病毒藥相比，favipiravir的作用機(jī)制是新穎的，主要能阻止病毒從細(xì)胞中進(jìn)入和退出。活性的favipiravir-RTP選擇性抑制RNA聚合酶并阻止病毒基因組的復(fù)制。目前有幾種假設(shè)favipiravir-RTP如何與RNA依賴性RNA聚合酶（RdRp）相互作用。一些研究表明，將favipiravir-RTP摻入新生的RNA鏈中時，它會阻止RNA鏈延長和病毒增殖。7研究還發(fā)現(xiàn)， 嘌呤類似物可以降低favipiravir的抗病毒活性，表明favipiravir-RTP和嘌呤核苷之間存在RdRp結(jié)合競爭7。
盡管favipiravir最初是開發(fā)用于治療流感的，但預(yù)計RdRp催化域（favipiravir的主要靶標(biāo)）與其他RNA病毒相似。這種保守的RdRp催化域有助于favipiravir的廣譜覆蓋。
transcription of virus RNA segments. The transcription of viral mRNAs occurs by a unique mechanism called cap-snatching. 5' methylated caps of cellular mRNAs are cleaved after 10-13 nucleotides by PA. In turn, these short capped RNAs are used as primers by PB1 for transcription of viral mRNAs. During virus replication, PB1 initiates RNA synthesis and copy vRNA into complementary RNA (cRNA) which in turn serves as a template for the production of more vRNAs.Favipiravir shows anti-influenza virus activities with IC50 ranged from 0.013 to 0.48 μg/ml for the influenza A viruses, from 0.039 to 0.089 μg/ml for the influenza B viruses, and from 0.030 to 0.057 μg/ml for the influenza C viruses. In mammalian cell lines (MDCK cells, Vero cells, HEL cells, A549 cells, HeLa cells, and HEp-2 cells), Favipiravir shows no cytotoxicity at concentrations up to 1,000 μg/ml. In MDCK cells inoculated with seasonal influenza A (H1N1) viruses, Favipiravir induces lethal mutagenesis.
In repeat-dose toxicity studies involving dogs, rats, and monkeys, notable findings after administration of oral favipiravir included: adverse effects on hematopoietic tissues such as decreased red blood cell (RBC) production, and increases in liver function parameters such as aspartate aminotransferase (AST), alkaline phosphatase (ALP), alanine aminotransferase (ALT) and total bilirubin, and increased vacuolization in hepatocytes.18 Testis toxicity was also noted.18 Favipiravir is known to be teratogenic; therefore, administration of favipiravir should be avoided in women if pregnancy is confirmed or suspected.7,16 Toxicity information regarding favipiravir in humans is not readily available.
| Beigel J, Bray M: Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. doi: 10.1016/j.antiviral.2008.01.003. Epub 2008 Feb 4. [PubMed:18328578] |
| Hsieh HP, Hsu JT: Strategies of development of antiviral agents directed against influenza virus replication. Curr Pharm Des. 2007;13(34):3531-42. [PubMed:18220789] |
| Gowen BB, Wong MH, Jung KH, Sanders AB, Mendenhall M, Bailey KW, Furuta Y, Sidwell RW: In vitro and in vivo activities of T-705 against arenavirus and bunyavirus infections. Antimicrob Agents Chemother. 2007 Sep;51(9):3168-76. Epub 2007 Jul 2. [PubMed:17606691] |
| Sidwell RW, Barnard DL, Day CW, Smee DF, Bailey KW, Wong MH, Morrey JD, Furuta Y: Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice. Antimicrob Agents Chemother. 2007 Mar;51(3):845-51. Epub 2006 Dec 28. [PubMed:17194832] |
| Furuta Y, Takahashi K, Kuno-Maekawa M, Sangawa H, Uehara S, Kozaki K, Nomura N, Egawa H, Shiraki K: Mechanism of action of T-705 against influenza virus. Antimicrob Agents Chemother. 2005 Mar;49(3):981-6. [PubMed:15728892] |
Beigel J, Bray M: Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. doi: 10.1016/j.antiviral.2008.01.003. Epub 2008 Feb 4.
Beigel J, Bray M: Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. doi: 10.1016/j.antiviral.2008.01.003. Epub 2008 Feb 4.
Hsieh HP, Hsu JT: Strategies of development of antiviral agents directed against influenza virus replication. Curr Pharm Des. 2007;13(34):3531-42.
Gowen BB, Wong MH, Jung KH, Sanders AB, Mendenhall M, Bailey KW, Furuta Y, Sidwell RW: In vitro and in vivo activities of T-705 against arenavirus and bunyavirus infections. Antimicrob Agents Chemother. 2007 Sep;51(9):3168-76. Epub 2007 Jul 2.
Sidwell RW, Barnard DL, Day CW, Smee DF, Bailey KW, Wong MH, Morrey JD, Furuta Y: Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice. Antimicrob Agents Chemother. 2007 Mar;51(3):845-51. Epub 2006 Dec 28.
Furuta Y, Takahashi K, Kuno-Maekawa M, Sangawa H, Uehara S, Kozaki K, Nomura N, Egawa H, Shiraki K: Mechanism of action of T-705 against influenza virus. Antimicrob Agents Chemother. 2005 Mar;49(3):981-6.
Furuta Y, Takahashi K, Fukuda Y, Kuno M, Kamiyama T, Kozaki K, Nomura N, Egawa H, Minami S, Watanabe Y, Narita H, Shiraki K: In vitro and in vivo activities of anti-influenza virus compound T-705. Antimicrob Agents Chemother. 2002 Apr;46(4):977-81.
Furuta Y, Komeno T, Nakamura T: Favipiravir (T-705), a broad spectrum inhibitor of viral RNA polymerase. Proc Jpn Acad Ser B Phys Biol Sci. 2017;93(7):449-463. doi: 10.2183/pjab.93.027.
Venkataraman S, Prasad BVLS, Selvarajan R: RNA Dependent RNA Polymerases: Insights from Structure, Function and Evolution. Viruses. 2018 Feb 10;10(2). pii: v10020076. doi: 10.3390/v10020076.
Hayden FG, Shindo N: Influenza virus polymerase inhibitors in clinical development. Curr Opin Infect Dis. 2019 Apr;32(2):176-186. doi: 10.1097/QCO.0000000000000532.
Madelain V, Nguyen TH, Olivo A, de Lamballerie X, Guedj J, Taburet AM, Mentre F: Ebola Virus Infection: Review of the Pharmacokinetic and Pharmacodynamic Properties of Drugs Considered for Testing in Human Efficacy Trials. Clin Pharmacokinet. 2016 Aug;55(8):907-23. doi: 10.1007/s40262-015-0364-1.
Nguyen TH, Guedj J, Anglaret X, Laouenan C, Madelain V, Taburet AM, Baize S, Sissoko D, Pastorino B, Rodallec A, Piorkowski G, Carazo S, Conde MN, Gala JL, Bore JA, Carbonnelle C, Jacquot F, Raoul H, Malvy D, de Lamballerie X, Mentre F: Favipiravir pharmacokinetics in Ebola-Infected patients of the JIKI trial reveals concentrations lower than targeted. PLoS Negl Trop Dis. 2017 Feb 23;11(2):e0005389. doi: 10.1371/journal.pntd.0005389. eCollection 2017 Feb.
de Farias ST, Dos Santos Junior AP, Rego TG, Jose MV: Origin and Evolution of RNA-Dependent RNA Polymerase. Front Genet. 2017 Sep 20;8:125. doi: 10.3389/fgene.2017.00125. eCollection 2017.
Shu B, Gong P: Structural basis of viral RNA-dependent RNA polymerase catalysis and translocation. Proc Natl Acad Sci U S A. 2016 Jul 12;113(28):E4005-14. doi: 10.1073/pnas.1602591113. Epub 2016 Jun 23.
Nagata T, Lefor AK, Hasegawa M, Ishii M: Favipiravir: a new medication for the Ebola virus disease pandemic. Disaster Med Public Health Prep. 2015 Feb;9(1):79-81. doi: 10.1017/dmp.2014.151. Epub 2014 Dec 29.
Rosenke K, Feldmann H, Westover JB, Hanley PW, Martellaro C, Feldmann F, Saturday G, Lovaglio J, Scott DP, Furuta Y, Komeno T, Gowen BB, Safronetz D: Use of Favipiravir to Treat Lassa Virus Infection in Macaques. Emerg Infect Dis. 2018 Sep;24(9):1696-1699. doi: 10.3201/eid2409.180233. Epub 2018 Sep 17.
Delang L, Abdelnabi R, Neyts J: Favipiravir as a potential countermeasure against neglected and emerging RNA viruses. Antiviral Res. 2018 May;153:85-94. doi: 10.1016/j.antiviral.2018.03.003. Epub 2018 Mar 7.
Nature Biotechnology: Coronavirus puts drug repurposing on the fast track
Pharmaceuticals and Medical Devices Agency: Avigan (favipiravir) Review Report
World Health Organization: Influenza (Avian and other zoonotic)
Beigel J, Bray M: Current and future antiviral therapy of severe seasonal and avian influenza. Antiviral Res. 2008 Apr;78(1):91-102. doi: 10.1016/j.antiviral.2008.01.003. Epub 2008 Feb 4.
Hsieh HP, Hsu JT: Strategies of development of antiviral agents directed against influenza virus replication. Curr Pharm Des. 2007;13(34):3531-42.
Gowen BB, Wong MH, Jung KH, Sanders AB, Mendenhall M, Bailey KW, Furuta Y, Sidwell RW: In vitro and in vivo activities of T-705 against arenavirus and bunyavirus infections. Antimicrob Agents Chemother. 2007 Sep;51(9):3168-76. Epub 2007 Jul 2.
Sidwell RW, Barnard DL, Day CW, Smee DF, Bailey KW, Wong MH, Morrey JD, Furuta Y: Efficacy of orally administered T-705 on lethal avian influenza A (H5N1) virus infections in mice. Antimicrob Agents Chemother. 2007 Mar;51(3):845-51. Epub 2006 Dec 28.
Furuta Y, Takahashi K, Kuno-Maekawa M, Sangawa H, Uehara S, Kozaki K, Nomura N, Egawa H, Shiraki K: Mechanism of action of T-705 against influenza virus. Antimicrob Agents Chemother. 2005 Mar;49(3):981-6.
Furuta Y, Takahashi K, Fukuda Y, Kuno M, Kamiyama T, Kozaki K, Nomura N, Egawa H, Minami S, Watanabe Y, Narita H, Shiraki K: In vitro and in vivo activities of anti-influenza virus compound T-705. Antimicrob Agents Chemother. 2002 Apr;46(4):977-81.
Furuta Y, Komeno T, Nakamura T: Favipiravir (T-705), a broad spectrum inhibitor of viral RNA polymerase. Proc Jpn Acad Ser B Phys Biol Sci. 2017;93(7):449-463. doi: 10.2183/pjab.93.027.
Venkataraman S, Prasad BVLS, Selvarajan R: RNA Dependent RNA Polymerases: Insights from Structure, Function and Evolution. Viruses. 2018 Feb 10;10(2). pii: v10020076. doi: 10.3390/v10020076.
Hayden FG, Shindo N: Influenza virus polymerase inhibitors in clinical development. Curr Opin Infect Dis. 2019 Apr;32(2):176-186. doi: 10.1097/QCO.0000000000000532.
Madelain V, Nguyen TH, Olivo A, de Lamballerie X, Guedj J, Taburet AM, Mentre F: Ebola Virus Infection: Review of the Pharmacokinetic and Pharmacodynamic Properties of Drugs Considered for Testing in Human Efficacy Trials. Clin Pharmacokinet. 2016 Aug;55(8):907-23. doi: 10.1007/s40262-015-0364-1.
Nguyen TH, Guedj J, Anglaret X, Laouenan C, Madelain V, Taburet AM, Baize S, Sissoko D, Pastorino B, Rodallec A, Piorkowski G, Carazo S, Conde MN, Gala JL, Bore JA, Carbonnelle C, Jacquot F, Raoul H, Malvy D, de Lamballerie X, Mentre F: Favipiravir pharmacokinetics in Ebola-Infected patients of the JIKI trial reveals concentrations lower than targeted. PLoS Negl Trop Dis. 2017 Feb 23;11(2):e0005389. doi: 10.1371/journal.pntd.0005389. eCollection 2017 Feb.
de Farias ST, Dos Santos Junior AP, Rego TG, Jose MV: Origin and Evolution of RNA-Dependent RNA Polymerase. Front Genet. 2017 Sep 20;8:125. doi: 10.3389/fgene.2017.00125. eCollection 2017.
Shu B, Gong P: Structural basis of viral RNA-dependent RNA polymerase catalysis and translocation. Proc Natl Acad Sci U S A. 2016 Jul 12;113(28):E4005-14. doi: 10.1073/pnas.1602591113. Epub 2016 Jun 23.
Nagata T, Lefor AK, Hasegawa M, Ishii M: Favipiravir: a new medication for the Ebola virus disease pandemic. Disaster Med Public Health Prep. 2015 Feb;9(1):79-81. doi: 10.1017/dmp.2014.151. Epub 2014 Dec 29.
Rosenke K, Feldmann H, Westover JB, Hanley PW, Martellaro C, Feldmann F, Saturday G, Lovaglio J, Scott DP, Furuta Y, Komeno T, Gowen BB, Safronetz D: Use of Favipiravir to Treat Lassa Virus Infection in Macaques. Emerg Infect Dis. 2018 Sep;24(9):1696-1699. doi: 10.3201/eid2409.180233. Epub 2018 Sep 17.
Delang L, Abdelnabi R, Neyts J: Favipiravir as a potential countermeasure against neglected and emerging RNA viruses. Antiviral Res. 2018 May;153:85-94. doi: 10.1016/j.antiviral.2018.03.003. Epub 2018 Mar 7.
Nature Biotechnology: Coronavirus puts drug repurposing on the fast track
Pharmaceuticals and Medical Devices Agency: Avigan (favipiravir) Review Report
World Health Organization: Influenza (Avian and other zoonotic)
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