{"id":28103,"date":"2021-07-01T14:00:38","date_gmt":"2021-07-01T06:00:38","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=28103"},"modified":"2022-07-19T14:09:31","modified_gmt":"2022-07-19T06:09:31","slug":"%e7%91%9e%e5%be%b7%e8%a5%bf%e9%9f%8bremdesivir-a-nucleoside-analogue-with-antiviral-activity%e8%b2%a8%e8%99%9f-b2997","status":"publish","type":"post","link":"http:\/\/biopioneer.com.tw\/?p=28103","title":{"rendered":"\u745e\u5fb7\u897f\u97cb(Remdesivir) | A nucleoside analogue with antiviral activity\u8ca8\u865f B2997"},"content":{"rendered":"

\u745e\u5fb7\u897f\u97cb(Remdesivir) | A nucleoside analogue with antiviral activity<\/em><\/strong>\u8ca8\u865f<\/strong>\u00a0<\/strong>B2997<\/strong><\/a><\/span><\/p>\n

2019 \u65b0\u578b\u51a0\u72c0\u75c5\u6bd2 (SARS-CoV-2)\u767c\u5c55<\/p>\n

\u51a0\u72c0\u75c5\u6bd2 (Coronaviruses, \u00a0CoV) \u662f\u6709\u5305\u819c(enveloped)\u7684\u6b63\u93c8 RNA \u75c5\u6bd2(positive-sense RNA viruses)\uff0c\u5176\u7279\u5fb5\u662f\u5f9e\u5176\u8868\u9762\u4f38\u200b\u200b\u51fa\u7684\u51a0\u72c0\u5c16\u523a(crown-like spikes)\uff0c\u9019\u662f\u4e00\u7a2e\u7570\u5e38\u5927\u7684 RNA \u57fa\u56e0\u7d44(RNA genome)\u3002\u5b83\u5011\u5728\u4e0d\u540c\u7a2e\u985e\u7684\u52d5\u7269\u4e2d\u5f15\u8d77\u5404\u7a2e\u75be\u75c5\uff0c\u5305\u62ec\u99f1\u99dd(camels)\u3001\u725b(cattle)\u3001\u8c93(cats)\u548c\u8759\u8760(bats)\uff0c\u4e26\u5728\u4eba\u985e\u4e2d\u5f15\u8d77\u6f5b\u5728\u7684\u81f4\u547d\u547c\u5438\u9053\u611f\u67d3(lethal respiratory infections)\u3002\u4e2d\u6771\u547c\u5438\u7d9c\u5408\u5fb5\u51a0\u72c0\u75c5\u6bd2 (MERS-CoV) \u548c\u56b4\u91cd\u6025\u6027\u547c\u5438\u7d9c\u5408\u5fb5\u51a0\u72c0\u75c5\u6bd2 (SARS-CoV) \u662f\u5c0e\u81f4\u4eba\u985e\u56b4\u91cd\u547c\u5438\u7cfb\u7d71\u75be\u75c5\u7684\u516d\u7a2e\u5df2\u77e5\u4eba\u985e\u51a0\u72c0\u75c5\u6bd2\u4e4b\u4e00\u3002 SARS-CoV-2 \u662f\u5728\u4e2d\u570b\u6e56\u5317\u7701\u6b66\u6f22\u5e02\u767c\u73fe\u7684\u6700\u65b0\u51a0\u72c0\u75c5\u6bd2\u682a\u3002\u6700\u8fd1\uff0c\u7814\u7a76\u4eba\u54e1\u78ba\u5b9a\u4e86\u5728\u4e2d\u570b\u51fa\u73fe\u7684\u65b0\u578b\u51a0\u72c0\u75c5\u6bd2 (SARS-CoV-2) \u7684\u6574\u500b\u57fa\u56e0\u7d44\u5e8f\u5217\u3002 SARS-CoV-2 \u7684\u57fa\u56e0\u7d44\u5e8f\u5217\u8207 SARS-CoV \u7684\u76f8\u4f3c\u5ea6\u70ba 79%\uff0c\u8207 MERS-CoV \u7684\u76f8\u4f3c\u5ea6\u7d04\u70ba 51.8%\uff0c\u8207\u4f86\u81ea\u4e2d\u570b\u8759\u8760\u7684\u5176\u4ed6 SARS \u6a23\u51a0\u72c0\u75c5\u6bd2\u7684\u76f8\u4f3c\u5ea6\u7d04\u70ba 87%\u3002<\/p>\n

\u65b0\u51a0\u75c5\u6bd2(Coronavirus<\/strong>)\u3001\u8907\u88fd(Replication<\/strong>)\u3001\u767c\u75c5\u6a5f\u5236(Pathogenesis<\/strong>)\u548c\u6f5b\u5728\u7684\u6cbb\u7642\u85e5\u7269(Potential Therapeutic Agents<\/strong>)\uff1a<\/p>\n

\u51a0\u72c0\u75c5\u6bd2(Coronavirus<\/strong>)\u5305\u542b\u4e00\u500b\u7d04 30 kb \u7684\u975e\u5206\u6bb5\u7684\u6b63\u93c8 RNA \u57fa\u56e0\u7d44(non-segmented, positive-sense RNA genome)\u3002\u51a0\u72c0\u75c5\u6bd2\u75c5\u6bd2\u9846\u7c92(. Coronavirus virus particles)\u5305\u542b\u56db\u7a2e\u4e3b\u8981\u7d50\u69cb\u86cb\u767d(structural proteins)\u3002\u5b83\u5011\u662f\u523a\u7a81 (spike , S)\u3001\u819c (membrane , M)\u3001\u5305\u819c (envelope , E) \u548c\u6838\u8863\u6bbc (nucleocapsid ,N) \u86cb\u767d\uff0c\u6240\u6709\u9019\u4e9b\u86cb\u767d\u90fd\u5728\u75c5\u6bd2\u57fa\u56e0\u7d44\u7684 3′ \u7aef\u7de8\u78bc\u3002\u523a\u7a81\u7cd6\u86cb\u767d(spike glycoprotein)\u4ecb\u5c0e\u75c5\u6bd2\u9032\u5165\uff0c\u662f\u7d30\u80de\u8da8\u5411\u6027(cell tropism)\u548c\u767c\u75c5\u6a5f\u5236(pathogenesis)\u7684\u4e3b\u8981\u6c7a\u5b9a\u56e0\u7d20\u3002\u5b83\u88ab\u6b78\u985e\u70ba I \u985e\u878d\u5408\u86cb\u767d(class I fusion protein)\uff0c\u8ca0\u8cac\u8207\u5bbf\u4e3b\u7d30\u80de\u4e0a\u7684\u53d7\u9ad4\u7d50\u5408\u3002\u6b64\u5916\uff0c\u5b83\u4ecb\u5c0e\u5bbf\u4e3b\u548c\u75c5\u6bd2\u819c(viral membranes)\u7684\u878d\u5408\uff0c\u9019\u4e00\u904e\u7a0b\u7531 S \u86cb\u767d\u7684\u4e3b\u8981\u69cb\u8c61\u8b8a\u5316\u9a45\u52d5\u3002\u7531\u65bc S \u86cb\u767d(receptor recognition)\u53c3\u8207\u53d7\u9ad4\u8b58\u5225\u4ee5\u53ca\u75c5\u6bd2\u9644\u8457\u548c\u9032\u5165\uff0c\u56e0\u6b64\u5b83\u4ee3\u8868\u4e86\u958b\u767c\u75ab\u82d7(vaccines)\u548c\u6cbb\u7642\u65b9\u6cd5(therapeutics)\u7684\u6700\u91cd\u8981\u76ee\u6a19\u4e4b\u4e00\u3002spike\u4e5f\u662f\u4e2d\u548c\u6297\u9ad4\u7684\u4e3b\u8981\u76ee\u6a19\u3002\u6700\u8fd1\u7684 SARS-CoV-2 \u7206\u767c\u523a\u6fc0\u4e86\u5c0d CoV \u75c5\u6bd2\u7684\u7814\u7a76\uff0c\u9019\u9805\u7814\u7a76\u5df2\u7d93\u78ba\u5b9a\u4e86\u5927\u91cf\u5408\u9069\u7684\u6297\u75c5\u6bd2\u9776\u9ede\uff0c\u4f8b\u5982\u75c5\u6bd2\u86cb\u767d\u9176(viral proteases)\u3001\u805a\u5408\u9176(polymerases)\u548c\u9032\u5165\u86cb\u767d(entry proteins)\u3002\u7136\u800c\uff0c\u4ecd\u7136\u9700\u8981\u5927\u91cf\u7814\u7a76\u4f86\u958b\u767c\u91dd\u5c0d\u9019\u4e9b\u904e\u7a0b\u4e26\u53ef\u4ee5\u6291\u5236\u75c5\u6bd2\u8907\u88fd(inhibit viral replication)\u7684\u85e5\u7269\u3002<\/p>\n

SARS-CoV \u662f\u4e00\u7a2e\u6709\u5305\u819c(enveloped)\u7684\u55ae\u93c8\u6b63\u93c8 RNA \u75c5\u6bd2(positive-stranded RNA virus)\u3002\u56b4\u91cd\u6025\u6027\u547c\u5438\u7cfb\u7d71\u7d9c\u5408\u75c7\u51a0\u72c0\u75c5\u6bd2 (SARS-CoV) \u7684\u7d30\u80de\u9032\u5165\u7531\u75c5\u6bd2\u523a\u7a81 (S) \u86cb\u767d(viral spike (S) protein)\u4ecb\u5c0e\u3002\u5df2\u77e5\u51a0\u72c0\u75c5\u6bd2\u7684\u523a\u7a81 (spike (S) glycoprotein , S) \u7cd6\u86cb\u767d\u5728\u611f\u67d3\u904e\u7a0b\u958b\u59cb\u6642\u5c0d\u75c5\u6bd2\u8207\u5bbf\u4e3b\u7d30\u80de\u7684\u7d50\u5408\u81f3\u95dc\u91cd\u8981\u3002\u523a\u7a81\u86cb\u767d(spike protein)\u662f\u4e00\u7a2e\u5927\u578b I \u578b\u8de8\u819c\u86cb\u767d(large type I transmembrane protein)\uff0c\u5305\u542b\u5169\u500b\u4e9e\u57fa(two subunits) S1 \u548c S2\u3002\u5c0d\u65bc\u75c5\u6bd2\u9032\u5165\uff0cSARS S \u7684\u8868\u9762\u55ae\u5143 (surface unit , S1) \u8207\u7d30\u80de\u53d7\u9ad4\u8840\u7ba1\u7dca\u5f35\u7d20\u8f49\u5316\u9176 2 (cellular receptor angiotensin converting enzyme 2, ACE2) \u7d50\u5408\uff0c\u7136\u5f8c\u8de8\u819c\u55ae\u5143 (transmembrane protein , S2) \u5c07\u75c5\u6bd2\u819c\u8207\u5bbf\u4e3b\u7d30\u80de\u819c\u878d\u5408\u3002\u5728\u611f\u67d3 SARS-CoV \u671f\u9593\uff0cS \u86cb\u767d(S protein)\u5728\u8a98\u5c0e\u4e2d\u548c\u6297\u9ad4(neutralizing-antibody)\u548c T \u7d30\u80de\u53cd\u61c9(T-cell responses)\u4ee5\u53ca\u4fdd\u8b77\u6027\u514d\u75ab\u4e2d\u8d77\u8457\u95dc\u9375\u4f5c\u7528\u3002\u7531\u65bc SARS-CoV \u7684 S \u86cb\u767d(S protein)\u53c3\u8207\u53d7\u9ad4\u8b58\u5225(receptor recognition)\u4ee5\u53ca\u75c5\u6bd2\u9644\u8457\u548c\u9032\u5165(virus attachment and entry)\uff0c\u56e0\u6b64\u5b83\u4ee3\u8868\u4e86 SARS \u75ab\u82d7\u548c\u7642\u6cd5\u958b\u767c\u7684\u6700\u91cd\u8981\u9776\u9ede\u4e4b\u4e00\u3002<\/p>\n

 <\/p>\n

BioVision \u63d0\u4f9b\u591a\u7a2e\u7522\u54c1\u4f86\u652f\u6301\u51a0\u72c0\u75c5\u6bd2\u7814\u7a76\uff0c\u5305\u62ec\u6aa2\u6e2c\u8a66\u5291\u76d2\u3001\u6297\u9ad4\u3001\u86cb\u767d\u8cea\u3001\u751f\u7269\u5316\u5b78\u54c1\u548c\u8a31\u591a\u96dc\u9805\u7522\u54c1\uff0c\u63d0\u4f9b\u51a0\u72c0\u75c5\u6bd2\u7814\u7a76\u7684\u7522\u54c1\u3002<\/p>\n

\u745e\u5fb7\u897f\u97cb(Remdesivir)\u7522\u54c1\u4ecb\u7d39:<\/strong><\/p>\n

\"\"<\/p>\n

\u745e\u5fb7\u897f\u97cb(Remdesivir)\u662f\u4e00\u7a2e\u5177\u6709\u6297\u75c5\u6bd2\u6d3b\u6027(antiviral activity)\u7684\u6838\u82f7\u985e\u4f3c\u7269(nucleoside analogue)\u3002\u5b83\u6291\u5236\u4e2d\u6771\u547c\u5438\u7d9c\u5408\u5fb5\u51a0\u72c0\u75c5\u6bd2 (Middle East respiratory syndrome coronavirus, MERS-CoV) \u6216\u56b4\u91cd\u6025\u6027\u547c\u5438\u7d9c\u5408\u5fb5\u51a0\u72c0\u75c5\u6bd2 (severe acute respiratory syndrome coronavirus , SARS-CoV) \u611f\u67d3\u7684 HAE \u57f9\u990a\u7269\uff0cEC\u2085\u2080 \u503c\u70ba 74 nM \u548c 69 nM\u3002\u5b83\u5728\u5ef6\u9072\u8166\u816b\u7624 (delayed brain tumor ,DBT) \u7d30\u80de\u4e2d\u4ee5 30 nM \u7684 EC\u2085\u2080 \u6291\u5236\u9f20\u809d\u708e\u75c5\u6bd2 (MHV)\u3002\u5b83\u662f\u4e00\u7a2e\u5ef6\u9072\u93c8\u7d42\u6b62\u5291(delayed chain terminator)\uff0c\u5177\u6709\u91dd\u5c0d\u591a\u7a2e\u51a0\u72c0\u75c5\u6bd2(multiple coronaviruses)\u7684\u9ad4\u5916(in vitro)\u548c\u52d5\u7269\u6a21\u578b(animal model)\u6d3b\u6027\uff0c\u4ee5\u53ca\u200b\u200b\u91dd\u5c0d SARS-CoV-2 \u7684\u9ad4\u5916\u6d3b\u6027(in vitro activity)\u3002<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Alternate Name<\/strong><\/td>\n2-Ethylbutyl (2S)-2-(((S)-(((2R,3S,4R,5R)-5-(4-aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate; 2-ethylbutyl ((((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)-L-alaninate; GS-5734<\/td>\n<\/tr>\n
Appearance<\/strong><\/td>\nWhite to off-White crystalline powder<\/td>\n<\/tr>\n
CAS #<\/strong><\/td>\n1809249-37-3<\/td>\n<\/tr>\n
Molecular Formula<\/strong><\/td>\nC\u2082\u2087H\u2083\u2085N\u2086O\u2088P<\/td>\n<\/tr>\n
Molecular Weight<\/strong><\/td>\n602.58<\/td>\n<\/tr>\n
Purity<\/strong><\/td>\n>97%<\/td>\n<\/tr>\n
Solubility<\/strong><\/td>\n~125 mg\/ml in DMSO<\/td>\n<\/tr>\n
SMILES<\/strong><\/td>\nCCC(CC)COC(=O)C(C)NP(=O)(OCC1C(C(C(O1)(C#N)C2=CC=C3N2N=CN=C3N)O)O)OC4=CC=CC=C4<\/td>\n<\/tr>\n
InChi<\/strong><\/td>\nInChI=1S\/C27H35N6O8P\/c1-4-18(5-2)13-38-26(36)17(3)32-42(37,41-19-9-7-6-8-10-19)39-14-21-23(34)24(35)27(15-28,40-21)22-12-11-20-25(29)30-16-31-33(20)22\/h6-12,16-18,21,23-24,34-35H,4-5,13-14H2,1-3H3,(H,32,37)<\/td>\n<\/tr>\n
InChi Key<\/strong><\/td>\nRWWYLEGWBNMMLJ-YSOARWBDSA-N<\/td>\n<\/tr>\n
PubChem CID<\/strong><\/td>\n121304016<\/td>\n<\/tr>\n
MDL Number<\/strong><\/td>\nMFCD31657351<\/td>\n<\/tr>\n
Handling<\/strong><\/td>\nDo not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.<\/td>\n<\/tr>\n
Storage Conditions<\/strong><\/td>\n-20\u00baC<\/td>\n<\/tr>\n
Shipping Conditions<\/strong><\/td>\nRT<\/td>\n<\/tr>\n
USAGE<\/strong><\/td>\nFor Research Use Only! Not For Use in Humans.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

\u6297ACE2\u6297\u9ad4<\/a> |<\/p>\n

 <\/p>\n

 <\/p>\n

\u00a0<\/strong><\/p>\n","protected":false},"excerpt":{"rendered":"

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