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別名: NSC-163039, RTCA, Tribavirin 中文名稱:利巴韋林
Ribavirin (NSC-163039, ICN-1229, RTCA, Tribavirin)是一種抗病毒劑,用于治療重癥RSV感染,丙型肝炎病毒感染和其他病毒感染。
Ribavirin (ICN-1229) Chemical Structure
CAS: 36791-04-5
相關產(chǎn)品 | Moroxydine HCl Aloperine GS-441524 Oleanolic Acid NGI-1 Lapachol Saikosaponin B2 Harringtonine U18666A | 點擊展開 |
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相關化合物庫 | 抗感染化合物庫 抗生素化合物庫 抗病毒化合物庫 抗寄生蟲藥物庫 腸道微生物代謝物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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human KB cells | Function assay | 1-1000 μg/ml | 72 h | Antiviral activity against Rhinovirus type 13 infected in human KB cells assessed as inhibition of virus-induced cytopathic effect at 1 to 1000 ug/ml after 72 hrs | 211234 |
MDCK cells | Function assay | 3 days | Antiviral activity against Influenza B virus (B/HK/5/72) infected in MDCK cells assessed as virus-induced cytopathic effect after 3 days by microscopic analysis, EC50=0.094 μM | 23117173 | |
mouse L1210 cells | Function assay | 20-60 mins | Inhibition of IMPDH in mouse L1210 cells assessed as formation of [2,8-3H]hypoxanthine from [2,8-3H]IMP after 20 to 60 mins, IC50=1 μM | 22555152 | |
human CEM cells | Function assay | 20-60 mins | Inhibition of IMPDH in human CEM cells assessed as formation of [2,8-3H]hypoxanthine from [2,8-3H]IMP after 20 to 60 mins, IC50=1 μM | 22555152 | |
MDCK cells | Function assay | 36 h | Antiinfluenza activity against influenza A virus H1N1 infected in MDCK cells assessed as inhibition of virus-induced cytopathic effect after 36 hrs, IC50=1.9 μM | 22341943 | |
MDBK cells | Function assay | 2 days | Antiviral activity against Bovine viral diarrhea virus 1-NADL ATCC VR534 infected in MDBK cells assessed as reduction of viral cytopathic effect after 2 days bt MTS assay, EC50=4.6 μM | 22944333 | |
african green monkey Vero cells | Function assay | 5 days | Antiviral activity against RSV A2 infected in african green monkey Vero cells after 5 days by plaque reduction assay, EC50=7 μM | 20359898 | |
HEL cells | Function assay | 2-3 days | Antiviral activity against Herpes simplex virus 1 KOS infected in HEL cells assessed as protection from virus-induced cytopathogenicity after 2 to 3 days by MTT assay, EC50=10 μM | 20034711 | |
HEK293 cells | Function assay | 24 h | Inhibition of influenza A virus RNA-dependent RNA polymerase expressed in HEK293 cells after 24 hrs by dual luciferase reporter gene assay, EC50=15 μM | 24313730 | |
human BE(2)-C cells | Function assay | 18-20 h | Antiviral activity against Western equine encephalomyelitis virus infected in human BE(2)-C cells assessed as inhibition of viral RNA replication after 18 to 20 hrs by luciferase reporter gene assay, IC50=16 μM | 24151954 | |
human MT4 cells | Cytotoxic?assay | 96 h | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay, CC50=31 μM | 19482481 | |
human HuH7 cells | Cytotoxic?assay | 3 days | Cytotoxicity against human HuH7 cells infected with HCV1b after 3 days by MTS assay, CC50=32 μM | 22100256 | |
human KB cells | Function assay | 72 h | Antiviral activity against Rhinovirus type 13 infected in human KB cells assessed as inhibition of virus-induced cytopathic effect after 72 hrs relative to control | 722730 | |
E6SM cell lines | Function assay | Effective concentration required to inhibit Herpes simplex virus-1(HSV-1) / thymine kinase deficient (TK-)B2006 / VMW1837 induced cytopathicity by 50% in E6SM cell lines, EC50=0.005 μM | 11495586 | ||
BHK21 cell line | Function assay | Inhibition of West Nile virus VLP replicon in BHK21 cell line, EC50=1.1 μM | 16539402 | ||
HeLa cell | Function assay | Effective concentration required to inhibit respiratory synaptial(RSV) virus-induced cytopathicity by 50% in HeLa cell lines, EC50=1.5 μM | 11495586 | ||
human HuH7-J20 cells | Function assay | Antiviral activity against HCV JFH1 infected in human HuH7-J20 cells assessed as inhibition of viral life cycle by measuring secreted alkaline phosphatase level preincubated with cells for 1 hr followed by viral inoculation for 3 hrs measured at 72 hrs, EC50=30.4 μM | 26428870 | ||
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產(chǎn)品描述 | Ribavirin (NSC-163039, ICN-1229, RTCA, Tribavirin)是一種抗病毒劑,用于治療重癥RSV感染,丙型肝炎病毒感染和其他病毒感染。 |
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體外研究(In Vitro) | ||||
體外研究活性 | Ribavirin顯著降低了亞基因組復制子轉(zhuǎn)染細胞的復制系統(tǒng)的效率,盡管Ribavirin對HCV復制的水平幾乎沒有影響。Ribavirin增加丙型肝炎病毒的突變頻率,NS5A編碼區(qū)的突變率最高。Ribavirin增強TH1,同時抑制T2細胞因子產(chǎn)生刺激的T細胞。[1] Ribavirin顯示了抗病毒活性,抗多種RNA病毒,并結合使用α-干擾素來治療丙型肝炎病毒感染。Ribavirin減少感染的脊髓灰質(zhì)炎病毒的產(chǎn)生,少到細胞培養(yǎng)物的0.00001%。 [2] Ribavirin的抗病毒活性是通過病毒的遺傳物質(zhì)的致死突變直接作用。[3] Ribavirin在生理濃度(高達500毫克/毫升)顯著降低病毒引起的巨噬細胞的活化。Ribavirin抑制Th2細胞產(chǎn)生IL-4,而這并不會抹殺Th1細胞產(chǎn)生IFN-γ。[4] Ribavirin在體外表現(xiàn)出對DNA和RNA病毒廣泛的抗病毒活性。Ribavirin是一種細胞生長抑制劑,導致DNA,RNA和蛋白質(zhì)合成的的減少。Ribavirin能誘導輔助性T細胞表型從從2型轉(zhuǎn)變?yōu)?型。 [5] | |||
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | p53 / p-p53 / p21 / Mdm2 EZH2 / p-ERK / ERK / p-eIF4E / eIF4E / p21 Cyclin D1 p-AKT / AKT / pBP1 / BP1 |
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22962590 | |
Growth inhibition assay | Cell number |
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21415224 |
NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT05940545 | Recruiting | CCHF |
Liverpool School of Tropical Medicine |
July 12 2023 | Phase 1|Phase 2 |
NCT04283513 | Not yet recruiting | Hemorrhagic Fever |
U.S. Army Medical Research and Development Command |
October 31 2022 | Phase 2 |
NCT04335123 | Completed | COVID-19 |
University of Kansas Medical Center |
April 4 2020 | Phase 1 |
NCT04285034 | Completed | Lassa Fever |
University of Oxford |
November 26 2019 | -- |
NCT03889106 | Terminated | Lassa Fever |
University of Oxford|National Institute for Health Research United Kingdom|Kenema Government Hospital|London School of Hygiene and Tropical Medicine|Public Health England |
March 1 2019 | -- |
NCT03585725 | Terminated | Follicular Lymphoma|Mantle Cell Lymphoma |
Weill Medical College of Cornell University|Memorial Sloan Kettering Cancer Center |
September 26 2018 | Early Phase 1 |
分子量 | 244.20864 | 分子式 | C8H12N4O5 |
CAS號 | 36791-04-5 | SDF | Download Ribavirin (ICN-1229) SDF |
Smiles | C1=NC(=NN1C2C(C(C(O2)CO)O)O)C(=O)N | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 49 mg/mL ( (200.64 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : 49 mg/mL (200.64 mM) Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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