OSELTAMIVIR POTTASIUM CARBOXYLATE BDBM50484773 Oseltamivir Potassium Carboxylate
Guanidino-Oseltamivir Carboxylicacid BDBM50028503 CHEMBL81717
BDBM5025 Oseltamivir ethyl (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate US10919856, POSITIVE CONTROL
GS4071 Oseltamivir carboxylate BDBM4994 CHEMBL674 (3R,4R,5S)-5-amino-4-acetamido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylic acid
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- ChEMBL_1541516 Inhibition of oseltamivir-resistant Influenza A virus H3N2 neuraminidase
- ChEMBL_1541517 Inhibition of oseltamivir-resistant Influenza A virus H3N2 neuraminidase E119V mutant
- ChEBML_1649827 Inhibition of human liver CES1 expressed in baculovirus infected sf9 cells using oseltamivir as substrate
- ChEMBL_1649827 Inhibition of human liver CES1 expressed in baculovirus infected sf9 cells using oseltamivir as substrate
- ChEMBL_1295475 Inhibition of oseltamivir-resistant Influenza A virus H1N1 B/55/08 neuraminidase by chemiluminescence based assay
- ChEMBL_819005 Inhibition of oseltamivir-resistant H1N1 swine influenza virus neuraminidase H274Y mutant using 4-MU-NANA as substrate by fluorescence assay
- ChEMBL_698045 Inhibition of oseltamivir-resistant H1N1 swine influenza virus neuraminidase H274Y mutant activity expressed in HEK293T cells after 2 hrs by spectrofluorometry
- Neuraminidase Inhibition Assay The 50% inhibitory concentration (IC50) determination was carried out by using a 96-well microtitre plate as an array of reaction vessels. In the first well,a 0.1-mM solution of oseltamivir carboxylate was prepared by mixing 90 μl of 33 mM MES pH 6.5 containing 4 mM CaCl2 and 10 μl of a 1-mM oseltamivir carboxylate stock solution. Starting from the solution contained in the first well, an in-plate 10-fold serial dilution was performed using 33 mM MES pH 6.5 containing 4 mM CaCl2 as dilution buffer obtaining a 7 points dilution curve, the last well in the vertical lane was used to obtain a negative control (no oseltamivir was added). At the end of the dilution process, each well contained 90 μl of solution. To each well, 25 μl of the enzyme stock solution were mixed with the oseltamivir solution and incubated for 2 h at 37°C. After the incubation time, 25 μl of 20 μM MUNANA were added. In the reaction mixtures, the final concentration of oseltamivir carboxylate spanned in the ranges 0.064 nM-64.2 μM. After incubating the plate for 5 h at 37°C, 50 μl of stop solution (0.1 M Glycine, pH 10.7 containing 25% ethanol) were added. The fluorescence of the solutions contained in each well was read with the Victor3 multi-label counter. For the determination of the of oseltamivir carboxylate against neuraminidase N3, the same procedure described above was used, except for the concentrationof the oseltamivir carboxylate stock solution which was 10 μM. In the reaction mixtures, the final concentration of oseltamivir carboxylate spanned in the ranges 0.64 pM-642 nM.
- ChEMBL_675041 Inhibition of oseltamivir-resistant Influenza A virus (A/California/08/2009(H1N1)) neuraminidase H274Y mutant expressed in human 293T cells after 30 mins by spectrofluorimetric analysis
- Neuraminidase Activity Assay Practically in a microtitre plate, 90 μl of 33 mM MES pH 6.5 containing 4 mM CaCl2 were dispensed in each well, except for the first well of each lane. In the first well of each vertical lane, 18 μl of 0.01 mM oseltamivir were mixed with 162 μl of 33 mM MES pH 6.5 containing 4 mM CaCl2. The solution was thoroughly mixed to obtain a 1-μM oseltamivir carboxylate solution. For each assay, a 90-μl aliquot of this solution was withdrawn from the first well and added to the second well in the same vertical lane obtaining a 2-fold diluted solution of oseltamivir. The 2-fold dilution process was continued up to the seventh well, while the eighth well used as blank (no inhibitor was added). At the end of the dilution process, each well contained 90 μl of solution. To each well, 25 μl of enzyme stock solution were added. After an incubation time of 2 h, 25 μl of MUNANA were added to each well, the final concentrations of oseltamivir carboxylate spanned the range 10-643 nM for N1 assay. After 30 min of incubation, 50 μl of stop solution were added to the first vertical lane, and the fluorescence was recorded. After an additional 30 min (60 min total), the stop solution was added to the second vertical lane and the fluorescence recorded. After additional 30 min (90 min total), the stop solution was added to the third vertical lane and the fluorescence recorded and so on. The experiment was performed in duplicate. For the determination of oseltamivir carboxylate Ki against N3, the same procedure described for N1 was used, except for the concentration of oseltamivir carboxylate stock solution which was 0.1 μM.
- ChEMBL_1292457 Inhibition of neuraminidase H274Y mutant in Oseltamivir-resistant Influenza A virus A/Berlin/55/08(H1N1) using Na-star as substrate preincubated for 10 to 30 mins followed by substrate addition measured after 10 to 30 mins by chemiluminescence-based assay
- ChEMBL_1584606 Inhibition of oseltamivir-resistant Influenza A virus A/WSN/1933(H1N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay
- ChEMBL_1584614 Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant wild type neuraminidase transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay
- ChEMBL_1584615 Inhibition of oseltamivir-resistant Influenza A virus A/Vietnam/1194/2004(H5N1) recombinant neuraminidase H275Y mutant transfected in HEK293 cells using MUNANA as substrate assessed as release of 4-methylumbelliferone preincubated for 10 mins followed by substrate addition measured after 15 mins by fluorometric assay
- NA Inhibition Assay NA inhibitory activity was determined by the commercial NA inhibitory screening kit (Beyotime Institute of Biotechnology, Jiangsu, China). The reaction mixture containing the buffer, NA enzyme, test compounds, or oseltamivir carboxylate (which was prepared according to literature method [Lindegårdh et al., J. Pharm. Biomed. Anal., 42:430-433]) and the substrate were incubated at 37°C. Terminate the reaction by adding 150 μL stop solution to all wells including the blank row. Read the plate within 20 min of adding stop solution detecting fluorescence using an excitation wavelength of 355 nm and an emission wavelength of 460 nm.
- Activity assay for influenza virus neuraminidase Experimental materials:NA (neuraminidase) solution: allantoic fluid of chicken embryo infected by influenza virus;Enzyme catalyzed reaction system: 330 mmol/L of MES buffer solution (pH 3.5); 200 μmol/L of fluorogenic substrate MUNANA (2′-(4-methylumbelliferyl)-α-D-N-acetylneuraminic acid);4 mmol/L of CaCl2 solution; Stop buffer: 14 mmol/L of NaOH solution (14 mmol/L, 83% ethanol); Oseltamivir: 1 mmol/L;Enzyme activity assay: NA solution (with different diluted concentration) 40 μl; MES (fatty acid methyl ester sulfonate) (330 mmol/L): 10 μl; CaCl2 (4 mmol/L): 10 μl; MUNANA (200 μmol/L): 10 μl; H2O: 30 μl; The above materials were mixed together and incubated for 15 minutes, and 150 μl of the stop buffer was added: EX=355 nm XM=460 nm.