Daclatasvir Dihydrochloride
Katrangan
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) minangka obat kuat lan aktif sacara lisan.Protein HCV NS5Ainhibitor karoEC50s sawetara 9-146 pM kanggomacem-macem genotipe replika HCV.Daclatasvir dihydrochloride uga apolipeptida pengangkut anion organik 1B (OATP1B)lanOATP1B3inhibitor karoIC50s saka 1,5 µM lan 3,27 µM, mungguh.
IC50& Target
EC50: 50 pM (genotipe replika HCV 1a), 9 pM (genotipe replika HCV 1b), 71 pM (genotipe replika HCV 2a), 146 pM (genotipe replika HCV 3a), 12 pM (genotipe replika HCV 33 pM) lan HCV replika genotipe 5a)[1]
Kd: 8 nM (NS5A33-202) lan 210 nM (NS5A26-202)[2]
IC50: 1,5 µM (OATP1B) lan 3,27 µM (OATP1B3)[3]
Ing Vitro
Daclatasvir (BMS-790052) nduduhake aktivitas hambat sing kuat marang kabeh genotipe sing diuji, kanthi EC50nilai kiro-kiro saka 9 pm kanggo 146 pm.Daclatasvir nyegah genotipe replika HCV 1a, 1b, 2a, 3a, 4a lan 5a kanthi EC50angka 50 pm, 9 pm, 71 pm, 146 pm, 12 pm lan 33 pm, mungguh.Daclatasvir minangka inhibitor kuat saka virus infèksi genotipe 2a JFH-1 sing replikasi ing kultur sel (EC50= 28 pm)[1].Daclatasvir (BMS-790052) ikatan erat karo NS5A33-202 lan NS5A26-202 karo Kds saka 8 nM lan 210 nM, mungguh[2].
Lumbung
bubuk | -20°C | 3 taun |
4°C | 2 taun | |
Ing solvent | -80°C | 6 wulan |
-20°C | 1 wulan |
Uji klinis
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