Daclatasvir dihydrochloride
Tlhaloso
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) e matla ebile e sebetsa ka molomo.HCV NS5A protheineinhibitor kaEC50s mefuta e fapaneng ya 9-146 pM bakeng samefuta e mengata ea HCV replicon genotypes.Daclatasvir dihydrochloride le eona ke aanion ea tlhaho e tsamaisang polypeptide 1B (OATP1B)leOATP1B3inhibitor kaIC50s ea 1.5 µM le 3.27 µM, ka ho latellana.
IC50& Sepheo
EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 3 pM) HCV replicon genotype 5a)[1]
Kd: 8 nM (NS5A33-202) le 210 nM (NS5A26-202)[2]
IC50: 1.5 µM (OATP1B) le 3.27 µM (OATP1B3)[3]
Ka Vitro
Daclatasvir (BMS-790052) e bonts'a ts'ebetso e matla ea thibelo ho li-genotype tsohle tse lekiloeng, ka EC.50boleng ho tloha ho 9pm ho isa ho 146 pM.Daclatasvir e thibela HCV replicon genotype 1a, 1b, 2a, 3a, 4a le 5a ka EC50boleng ba 50 pM, 9 pM, 71 pM, 146 pM, 12 pM le 33 pM, ka ho latellana.Daclatasvir ke inhibitor e matla ea kokoana e tšoaetsanoang ea JFH-1 genotype 2a e ikatisang ka setso sa lisele (EC50=28pm)[1].Daclatasvir (BMS-790052) e tlama ka thata ho NS5A33-202 le NS5A26-202 le Kds ea 8 nM le 210 nM, ka ho latellana[2].
Polokelo
Phofo | -20°C | 3 lilemo |
4°C | lilemo tse 2 | |
Ka solvent | -80°C | Likhoeli tse 6 |
-20°C | 1 khoeli |
Teko ea Tleliniki
Nomoro ea NCT | Motšehetsi | Boemo | Letsatsi la qalo | Mokhahlelo |
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Tlhahiso18Merero ea Tlhahlobo ea Boleng e amohetsoeng4, le6merero e tlas'a tumello.
Sistimi e tsoetseng pele ea boleng ba machaba e thehile motheo o tiileng oa thekiso.
Tlhokomelo ea boleng e tsamaisana le potoloho eohle ea bophelo ba sehlahisoa ho netefatsa boleng le phello ea kalafo.
Sehlopha sa Litaba tsa Taolo ea Setsebi se tšehetsa litlhoko tsa boleng nakong ea kopo le ngoliso.