Atazanavir ic50
Common Questions and Answers about Atazanavir ic50
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HBV replicating cells were treated with different dosages of Flavocoxid to determine the drug inhibitory concentrations (IC50). Treatment with Flavocoxid or ETV or with drugs combination started 3 hours after transfection and was renewed every other day for 5 days. Total HBV replicative intermediates, viral transcripts and cccDNA levels were evaluated in untreated and treated HepG2 cells by quantitative real-time PCR, Southern and Northern blots experiments.
efficacy ratio (CC50:IC50), which is sufficient for clinical development in HBV.
“We have almost three decades worth of experience in cyclosporine chemistry. Drawing upon this experience in structure-activity relationships, we have learned that relatively small and selective changes to the chemical structure of the cyclosporine backbone can have very dramatic consequences in pharmacology,” commented Dr. Foster.
Two compounds, proparacaine and chlorophyllide, were shown to reduce HBV levels 4- to 6-fold with an IC50 of 1 and 1.5 lM, respectively, and were selected for further study.
Tenofovir 300mg and Emtricitabine 200MG after 5hr from inccident early morning i meet another doctor he prescribe me TAB. Atazanavir 300mg and Ritonavir 100mg i get it after 24hr. After that i traked sex worker for blood sample after 30hr from inccident and tested for STD after a day i get her result that having HIV 1/2&P24 COMBO TEST INDEX VALUE 0.07,
HERPES SIMPLEX VIRUS 1+2IgM SERUM 1.36, HERPES SIMPLEX 1+2 IgG SERUM 29.30,CHLAMYDIA TRACHMATIS POSITIVE, CHLAMYDIA PNEUMONAE POSITIVE.
In a biochemical assay, GS-461203 inhibited the polymerase activity of the recombinant NS5B from HCV genotypes 1b, 2a, 3a and 4a with IC50 values ranging from 0.7 to 2.6 M. GS-461203 is neither an inhibitor of human DNA and RNA polymerases nor an inhibitor of mitochondrial RNA polymerase.
Antiviral Activity
In HCV replicon assays, the EC50 values of ledipasvir against full-length replicons from genotypes 1a and 1b were 0.031 nM and 0.004 nM, respectively.
Importantly, CRV431 was shown to have the widest selective index of any known cyclophilin inhibitor, calculated by CC50/IC50 ratio. This optimized selective index may correlate with a best-in-class therapeutic index, and therefore, enhanced clinical utility against HBV.
At high concentrations of ketoconazole, the conversion of squalene to methyl sterols was also inhibited. The inhibition of cholesterol synthesis was dose-dependent with an IC50 approximately 2.8 X 10(-8) M. In parallel to the inhibition of cholesterol synthesis, there was a reciprocal increase in methyl sterol production. The related imidazole antimycotic, clotrimazole, had similar effects, whereas the imidazole anesthetic, etomidate, had little effect on cholesterol synthesis.
Inhibition was quantified using recombinant green fluorescent protein expressing virus variants. The IC50 values were in the same range for ganciclovir-sensitive and ganciclovir-resistant human cytomegalovirus, as calculated with 5.8+/-0.4 microM and 6.9+/-0.2 microM, respectively. This indicated a strong antiviral potential and a lack of cross-resistance. The optimal antiviral concentrations of artesunate were separable from those inducing cytotoxicity.
141 nM (EC50, JFH1/3a-NS5A hybrid replicon) [1]
Target: HCV NS5A
in vitro: Against JFH1/3a-NS5A, DCV was more potent (EC(50) = 0.52 nM) than GS-5885 (EC(50) = 141 nM). DCV sensitivity was increased against JFH1/3a-NS5A-M28V (EC50 = 0.006 nM), A30V (EC(50) = 0.012 nM), and E92A (EC(50) = 0.004 nM) while the NS5A-A30K and -Y93H variants exhibited reduced sensitivity to DCV (EC50 values of 23 nM and 1120 nM, respectively) and to GS-5885 (EC50 values of 1770 nM and 4300 nM, respectively) [1].
Rather, ellagic acid blocks effectively HBeAg secretion in HepG2 2.2.15 cells (IC50=0.07 microg/ml). Since HBeAg is involved in immune tolerance during HBV infection, ellagic acid, a newly identified functional anti-HBV compound, may be a new candidate therapeutic against immune tolerance in HBV-infected individuals.
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