dCMP, 2′-Deoxycytidine 5′-monophosphate, ʻakika manuahi CAS:1032-65-1
Helu Helu | XD90549 |
inoa mea kūʻai | dCMP, 2'-Deoxycytidine 5'-monophosphate, ʻakika manuahi |
CAS | 1032-65-1 |
ʻĀpana Molekala | C9H14N3O7P |
Kaumaha Molecular | 307.20 |
Nā kikoʻī mālama | -15 a -20 °C |
Kānāwai Kūʻai Kūlike | 29349990 |
Huahana Huahana
Ka nana aku | Paʻa |
Hoʻāʻo | 99% |
ʻO ka Beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) he mea hoʻopaneʻe koʻikoʻi koʻikoʻi o ka maʻi hepatitis C (HCV) RNA synthesis ma Huh-7 replicon cell.No ka pale ʻana i ka HCV NS5B RNA polymerase, pono e phosphorylated ʻo PSI-6130 i ke ʻano 5'-triphosphate.Ua noiʻi ʻia ka phosphorylation o PSI-6130 a me ka inhibition o HCV NS5B.ʻO ka phosphorylation o PSI-6130 e ke kanaka recombinant 2'-deoxycytidine kinase (dCK) a me ka uridine-cytidine kinase 1 (UCK-1) ua ana ʻia me ka hoʻohana ʻana i kahi hopena spectrophotometric i hui ʻia.Ua hōʻike ʻia ʻo PSI-6130 he substrate no ka dCK maʻemaʻe, me kahi Km o 81 microM a me kahi kcat o 0.007 s-1, akā ʻaʻole ia he substrate no UCK-1.PSI-6130 monophosphate (PSI-6130-MP) ua efficiently phosphorylated i ka diphosphate a ma hope i ka triphosphate e recombinant kanaka UMP-CMP kinase a me nucleoside diphosphate kinase.Ua aʻo ʻia ka pale ʻana o nā ʻano ʻāhiu a me ka mutated (S282T) HCV NS5B RNA polymerases.Ka steady-state inhibition mau (Ki) no PSI-61 30 triphosphate (PSI-6130-TP) me ka wild-type enzyme he 4.3 microM.Loaʻa nā hopena like me 2'-C-methyladenosine triphosphate (Ki = 1.5 microM) a me 2'-C-methylcytidine triphosphate (Ki = 1.6 microM).ʻO NS5B me ka hoʻololi S282T, ka mea i ʻike ʻia e hāʻawi i ke kū'ē i ka 2'-C-methyladenosine, ua kāohi ʻia e PSI-6130-TP e like me ke ʻano hihiu.ʻO ka hoʻohui ʻana o PSI-6130-MP i loko o ka RNA catalyzed e NS5B RNA polymerase i hoʻomaʻemaʻe ʻia i hopena i ka pau ʻana o ke kaulahao.