I-dCMP, i-2'-Deoxycytidine 5'-monophosphate, i-asidi yamahhala CAS: 1032-65-1
Inombolo Yekhathalogu | XD90549 |
Igama lemveliso | I-dCMP, i-2'-Deoxycytidine 5'-monophosphate, i-asidi yamahhala |
CAS | 1032-65-1 |
Ifomula yeemolekyuli | I-C9H14N3O7P |
Ubunzima beMolekyuli | 307.20 |
Iinkcukacha zokuGcina | -15 ukuya -20 °C |
IKhowudi yoMrhumo eHarmonized | 29349990 |
Ukucaciswa kweMveliso
Imbonakalo | Iqinile |
Isivavanyi | 99% |
I-Beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) yi-inhibitor ethile enamandla ye-virus ye-hepatitis C (HCV) i-RNA synthesis kwiiseli ze-Huh-7 replicon.Ukuthintela i-HCV NS5B RNA polymerase, i-PSI-6130 kufuneka ibe yi-phosphorylated kwi-5'-triphosphate form.I-phosphorylation ye-PSI-6130 kunye nokuvinjelwa kwe-HCV NS5B yaphandwa.I-phosphorylation ye-PSI-6130 nge-recombinant human 2'-deoxycytidine kinase (dCK) kunye ne-uridine-cytidine kinase 1 (UCK-1) ilinganiswa ngokusebenzisa i-spectrophotometric reaction.I-PSI-6130 iboniswe njenge-substrate ye-dCK ecocekileyo, ene-Km ye-81 microM kunye ne-kcat ye-0.007 s-1, kodwa yayingeyona i-substrate ye-UCK-1.I-PSI-6130 i-monophosphate (PSI-6130-MP) yayisebenza ngokufanelekileyo i-phosphorylated kwi-diphosphate kwaye emva koko kwi-triphosphate ngokuphinda kuphinde kubekho i-UMP-CMP kinase yomntu kunye ne-nucleoside diphosphate kinase, ngokulandelanayo.Uthintelo lwe-wild-type kunye ne-muted (S282T) i-HCV NS5B RNA polymerases yaphononongwa.I-steady-state inhibition constant (Ki) ye-PSI-61 30 triphosphate (PSI-6130-TP) kunye ne-enzyme yohlobo lwasendle yayiyi-4.3 microM.Iziphumo ezifanayo zifunyenwe nge-2'-C-methyladenosine triphosphate (Ki = 1.5 microM) kunye ne-2'-C-methylcytidine triphosphate (Ki = 1.6 microM).I-NS5B kunye nokuguqulwa kwe-S282T, eyaziwayo ukuba inikeze ukuchasana ne-2'-C-methyladenosine, yayithintelwe yi-PSI-6130-TP ngokufanelekileyo njengohlobo lwasendle.Ukudityaniswa kwe-PSI-6130-MP kwi-RNA eyenziwe yi-NS5B RNA polymerase ecocekileyo ibangele ukupheliswa kwekhonkco.