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1985605-59-1
  • names:

    Baloxavir

  • CAS號(hào):

    1985605-59-1

    MDL Number: MFCD31619273
  • MF(分子式): C26H21F2NO4S MW(分子量): 481.51
  • EINECS: Reaxys Number:
  • Pubchem ID:124081876 Brand:BIOFOUNT
巴洛沙韋

巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)是流感帽依賴性核酸內(nèi)切酶的抑制劑,巴洛沙韋可用于治療A型和B型流感。Baloxavir一次性使用一次,與血清酶升高或臨床上明顯的肝損傷無(wú)關(guān)。巴洛沙韋用于治療甲型和乙型流感病毒感染的流感帽依賴性核酸內(nèi)切酶的選擇性抑制劑。

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HCC307873-0.5mg 0.5mg 97% ¥ 4655.00 ¥ 4655.00 4-7周
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中文別名 巴洛沙韋(1985605-59-1);巴洛沙韋酸;S-033447;(12aR)-12-[(11S)-7,8-二氟-6,11-二氫二苯并[b,e]噻庚英-11-基]-6,8-二氧代-3,4,6,8,12,12a-六氫-1H-[1,4]噁嗪并[3,4-c]吡啶并[2,1-f][1,2,4]三嗪-7-醇;
英文別名 Baloxavir(1985605-59-1);Baloxavir acid; BXA; Xofluza; (((12aR)-12-((11S)-7,8-difluoro-6,11-dihydrodibenzo(b,E)thiepin-11-yl)-6,8-dioxo-3,4,6,8,12,12ahexahydro-1H-(1,4)oxazino(3,4-C)pyrido(2,1-F)(1,2,4)triazin-7-yl)oxy)methyl methyl carbonate;10.1H-(1,4)oxazino(3,4-C)pyrido(2,1-F)(1,2,4)triazine-6,8-dione, 12-((11S)-7,8-difluoro-6,11-dihydrodibenzo(b,E)thiepin-11-yl)-3,4,12,12a-tetrahydro-7-hydroxy-, (12aR)-;baloxavir;baloxavir marboxil;Xofluza;
CAS號(hào) 1985605-59-1
Inchi nChI = 1S / C24H19F2N3O4S / c25-16-6-5-13-15(20(16)26)12-34-18-4-2-1-3-14(18)21(13)29-19- 11-33-10-9-27(19)24(32)22-23(31)17(30)7-8-28(22)29 / h1-8,19,21,31H,9-12H2 / t19-,21 + / m1 / s1
InchiKey FIDLLEYNNRGVFR-CTNGQTDRSA-N
分子式 Formula C26H21F2NO4S
分子量 Molecular Weight 481.51
溶解度Solubility
性狀 固體粉末
儲(chǔ)藏條件 Storage conditions storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)毒理性質(zhì):

In clinical trials, there was little evidence that baloxavir caused liver injury, either in the form of serum enzyme elevations or clinically apparent liver disease. A proportion of patients with acute influenza A may have minor serum enzyme elevations during the acute illness, but these are independent of therapy and do not appear to be exacerbated by baloxavir.

Likelihood score: E (unlikely cause of clinically apparent liver injury).


巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)實(shí)驗(yàn)注意事項(xiàng):
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡,穿戴防護(hù)服和口罩,佩戴手套,避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生,必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ),并交于專業(yè)生物廢氣物處理公司處理,以免造成環(huán)境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:巴洛沙韋試劑,巴洛沙韋雜質(zhì),巴洛沙韋中間體,巴洛沙韋密度,巴洛沙韋溶解度,巴洛沙韋旋光度,巴洛沙韋閃點(diǎn),巴洛沙韋熔點(diǎn),巴洛沙韋購(gòu)買,巴洛沙韋MSDS,
產(chǎn)品說(shuō)明 巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)可以作為藥物雜質(zhì)對(duì)照品以及生物醫(yī)藥類試劑。
Introduction巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)can be used as a reference substance for drug impurities and reagents,only for research.
Application1Baloxavir(Baloxavir acid)是甲型和乙型流感病毒聚合酶PA亞基內(nèi)的一種首創(chuàng),有效且選擇性的帽核苷酸核酸內(nèi)切酶(CEN)抑制劑。Baloxavir抑制病毒RNA的轉(zhuǎn)錄和復(fù)制,并具有強(qiáng)大的抗病毒活性。
Application2巴洛沙韋是用于治療甲型和乙型流感病毒感染的流感帽依賴性核酸內(nèi)切酶的選擇性抑制劑。
Application3
巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)藥理學(xué):
1、巴洛沙韋(1985605-59-1,Baloxavir)是流感帽依賴性核酸內(nèi)切酶的抑制劑,巴洛沙韋可用于治療A型和B型流感。Baloxavir一次性使用一次,與血清酶升高或臨床上明顯的肝損傷無(wú)關(guān)。
2、巴洛沙韋是抗病毒藥,巴洛沙韋用于預(yù)防或治療病毒性疾病的藥物。它們可能發(fā)揮作用的方式包括通過(guò)抑制病毒DNA聚合酶來(lái)防止病毒復(fù)制。與特定的細(xì)胞表面受體結(jié)合并抑制病毒滲透或脫殼;抑制病毒蛋白質(zhì)合成;或阻止病毒組裝的后期。
3、巴洛沙韋是酶抑制劑 ,巴洛沙韋與酶結(jié)合的化合物或試劑,可防止正常的底物-酶結(jié)合和催化反應(yīng)。
4、Baloxavir marboxil是一流的單劑量口服藥物,具有新穎的擬議作用機(jī)制,已證明對(duì)多種流感病毒具有功效,包括對(duì)耐oseltamivir耐藥株和禽毒株(H7N9,H5N1 )進(jìn)行非臨床研究。Baloxavir是一種聚合酶酸性,依賴于帽的核酸內(nèi)切酶抑制劑,可用于治療癥狀不超過(guò)48小時(shí)的12歲及以上的急性單純性流感。它通過(guò)結(jié)合兩個(gè)核酸內(nèi)切酶結(jié)合位點(diǎn)之一來(lái)阻斷病毒增殖,從而抑制了甲型流感病毒和乙型流感病毒株的mRNA合成。Baloxavir可以與含多價(jià)陽(yáng)離子的產(chǎn)物發(fā)生相互作用,從而降低其血漿濃度。
警示圖
危險(xiǎn)性 warning
危險(xiǎn)性警示 Not available
安全聲明 H303+H313+H333
安全防護(hù) P264+P280+P305+P351+P338+P337+P313
備注 實(shí)驗(yàn)過(guò)程中防止吸入、食入,做好安全防護(hù)
Omoto S, et al. Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil. Sci Rep. 2018 Jun 25;8(1):9633.
Noshi T, et al. In vitro characterization of baloxavir acid, a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit. Antiviral Res. 2018 Dec;160:109-117.
Baloxavir: First Global Approval PMID 29623652; Drugs 2018 Apr; 78(6):693-697 (Review Article) Name matches: baloxavir marboxil baloxavir
Marboxil CID 124081896 42 articles Download CSVView in PubMed Baloxavir: First Global Approval PMID 29623652; Drugs 2018 Apr; 78(6):693-697 (Review Article) Name matches: baloxavir marboxil baloxavir
Baloxavir: A Novel Antiviral Agent in the Treatment of Influenza PMID 32020174; Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 2020 Feb; ?(?): Nam
巴洛沙韋(1985605-59-1,Baloxavir,Baloxavir acid,S-033447)參考文獻(xiàn):
1、Modeling mitigation of influenza epidemics by baloxavir
Zhanwei Du, Ciara Nugent, Alison P. Galvani, Robert M. Krug & Lauren Ancel Meyers

Results and discussion Impact of antiviral treatment on the cell-to-cell proliferation of influenza Our within-host model assumes that infected patients have an initial load of drug-sensitive virus that increases via replication and decreases via immune response and antiviral treatment10,11 (Supplementary Fig. 1). We estimated the efficacy with which oseltamivir and baloxavir inhibit viral replication by fitting the model to the results of a recent clinical trial8 that measured the viral loads of 1014 influenza virus-infected patients after treatment with oseltamivir, baloxavir, or a placebo (Table 1). Our model produces viral titer estimates similar to the clinical data, and, like the clinical data, shows that baloxavir inhibits influenza virus replication more effectively than oseltamivir (Fig. 1). Within 1 day of initiating baloxavir or oseltamivir treatment, virus load decreases by an estimated 84% or 56%, respectively, compared with an expected reduction in untreated cases of 39%. The observed differences in the time between symptom onset and the initiation of treatment for patients in the clinical trial accounts for most of the observed variability in virus replication (Fig. 1, standard deviations). We used the fitted model to predict the effectiveness of drug treatment scenarios beyond those tested in the clinical trial, including the initiation of baloxavir or oseltamivir regimens at different times after symptom onset (Supplementary Fig. 3).

2、Baloxavir for the treatment of Influenza in allogeneic hematopoietic stem cell transplant recipients previously treated with oseltamivir
Mirella Salvatore 1, Jennifer M Laplante 2, Rosemary Soave 1, Nina Orfali 1, Markus Plate 1, Koen van Besien 3, Kirsten St George 2

Abstract Background: Seasonal influenza causes significant morbidity and mortality in allogeneic stem cell transplant (SCT) recipients. In this population, influenza virus can replicate for prolonged periods, despite neuraminidase inhibitor treatment, leading to resistance and treatment failure. Baloxavir targets the influenza polymerase and may be an effective treatment option in these patients. Methods: We used baloxavir to treat five allogeneic SCT recipients that were still symptomatic and shedding influenza virus after completing one or more treatment courses of oseltamivir and characterized the viral isolates before and during treatment. Results: Two patients were infected with influenza A/H1pdm09 carrying a neuraminidase variant (H275Y) linked to oseltamivir resistance. Both these two patients were successfully treated with baloxavir. Of the three patients infected with wild-type influenza virus, two cleared the virus after baloxavir treatment, while the third patient developed the polymerase I38T variant linked to baloxavir resistance. Conclusions: Our data suggest that baloxavir treatment can be effective in treating neuraminidase inhibitor-resistant influenza in profoundly immunocompromised patients. Randomized clinical trials are needed to define the role of baloxavir alone and combined with oseltamivir for the treatment of influenza in SCT recipients and other immunocompromised populations. Keywords: antiviral resistance; baloxavir marboxil; influenza A virus; neuraminidase inhibitors; oseltamivir; stem cell transplant.

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