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N-羥基胞苷 |
| CAS No.: |
3258-02-4 |
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| 備注： |
中文名稱N-羥基胞苷中文同義詞N-羥基胞苷;N-羥基胞苷(NHC(EIDD-1931));1-((2R,3R,4S,5R)-3,4-二羥基-5-(羥甲基)四氫呋喃-2-基)-4-(羥基亞氨基)-3,4-二氫嘧啶-2(1H)-酮;N-羥基胞苷(NHC);莫那比拉韋雜質(zhì)1;莫匹拉韋中EIDD-1931;莫匹拉韋中間體EIDD-1931;EIDD-1931N-羥基胞苷英文名稱N(4)-hydroxycytidine英文同義詞N(4)-hydroxycytidine;1-[(2R)-3α,4α-Dihydroxy-5β-(hydroxymethyl)oxolane-2β-yl]-4-(hydroxyamino)pyrimidine-2(1H)-one;3,4-Dihydro-1-β-D-ribofuranosyl-4-(hydroxyimino)pyrimidin-2(1H)-one;N-Hydroxycytidine;β-D-N4-Hydroxycytidine;Beta-d-N4-hydroxycytidine;EIDD-1931;Beta-d-N4-hydroxycytidine(NHC)CAS號(hào)3258-02-4分子式C9H13N3O6分子量259.22EINECS號(hào)相關(guān)類別芳香族;抑制劑;醫(yī)藥原料;化合物產(chǎn)品;化工原料;原料藥及中間體類;雜質(zhì)對(duì)照品;對(duì)照品Mol文件3258-02-4.mol結(jié)構(gòu)式N-羥基胞苷性質(zhì)熔點(diǎn)169-172°C(Solv:methanol(67-56-1))密度1.93±0.1g/cm3(Predicted)儲(chǔ)存條件Inertatmosphere,Storeinfreezer,under-20°C溶解度可溶于DMSO（高達(dá)25mg/ml）或水（加熱時(shí)高達(dá)15mg/ml）。形態(tài)固體酸度系數(shù)(pKa)8.19±0.20(Predicted)顏色白色穩(wěn)定性DMSO或蒸餾水中的溶液可在-20°下穩(wěn)定儲(chǔ)存3個(gè)月。N-羥基胞苷用途與合成方法生物活性EIDD-1931(Beta-d-N4-hydroxycytidine,β-d-N4-hydroxycytidine,NHC)是EIDD-2801的活性代謝產(chǎn)物，它是一種很有前途的COVID-19抑制劑。EIDD-1931（NHC）對(duì)ChemicalbookSARS-CoV-2、MERS-CoV、SARS-CoV和relatedzoonoticgroup2b或2cBat-CoVs，對(duì)應(yīng)的平均IC50值為0.15μM，并且對(duì)帶有對(duì)核苷類似物抑制劑remdesivir耐藥性突變的冠狀病毒的效力增強(qiáng)。體外研究Beta-d-N4-hydroxycytidineisananti-VEEV(venezuelanequineencephalitisvirus)agentwithEC50,EC90,andEC99are0.426,1.036,and2.5μM,respectively.Beta-d-N4-hydroxycytidineinhibitsCHIKVrepliconactivityandthe50%effectiveconcentration(EC50)s0.8μMintheHuh-7–CHIKVrepliconcellline.SimilarresultsispresentedwiththerepliconinBHK-21cells(EC50=1.8μM).NHChasnocytotoxicityforNHCintheHuh-7cellculturesystemuntilupto100μMusingMTTassays.The50%cytotoxicconcentration(CCsub>50)valuesforNHCaredeterminedtobe30.6μM,7.7μM,and2.5μMinperipheralbloodmononuclear(PBM),Vero,andCEMcells,respectively.NHCbehavesasapyrimidineanalog,NHC-mediatedinhibitionoftheCHIKVrepliconcanbeabrogatedbytheadditionofexogenousnucleosides,suchaspyrimidinesCandU,butdA,dC,dG,dU,orThasnoimpactonthereplicon.PyrimidinesAandGcontributestorepliconinhibitionbothinthepresenceandintheabsenceofNHC. |
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聯(lián)系人： |
金經(jīng)理 |
地 址： |
湖北省武漢市東湖新技術(shù)開發(fā)區(qū)光谷大道41號(hào) |
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430000 |
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18995560451 |
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15102708508 |
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18995560451 |
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