Fluconazole, supplied by Cayman Chemical, used in various techniques. Bioz Stars score: 91/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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1) Product Images from "Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations"
Article Title: Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations
Journal: Antimicrobial Agents and Chemotherapy
Figure Legend Snippet: In vitro evaluation of DB766-azole combinations against intracellular L. donovani . Posaconazole (POS; gray bars), ketoconazole (KTC; horizontal striped bars), or fluconazole (FLC; diagonal striped bars) was added to a serial dilution of DB766, with the azole at a fixed concentration, in at least three independent experiments. The concentrations of azole drugs employed were below those required for 50% inhibition alone (parasite burden was reduced by 39% ± 3% at 6.3 μM posaconazole alone [ n = 3], 23% ± 8% at 25 μM ketoconazole alone [ n = 3], and 14% ± 5% at 50 μM fluconazole alone [ n = 4]). Error bars and measurements represent the standard errors of the means. Two-sided Student's t test was used to compare the groups to the DB766-alone group. **, P
Techniques Used: In Vitro, Serial Dilution, Concentration Assay, Inhibition
Figure Legend Snippet: Structures of DB766, posaconazole, ketoconazole, and fluconazole.
2) Product Images from "CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)"
Article Title: CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)
Journal: PLoS Neglected Tropical Diseases
Figure Legend Snippet: NfCYP51-inhibitor binding. ( A ) Posaconazole ( yellow sticks ) and itraconazole ( black lines ) are shown overlapped. Fragment of the 1.7 Å 2F o -F c electron density map countered at 1.σ is shown for posaconazole ( cyan mesh ). Amino acid residues within 5 Å are in blue , heme is in spheres . Ketoconazole ( B ), voriconazole ( C ) and fluconazole ( D ) are shown in yellow sticks with the corresponding map fragments in cyan mesh . In C and D , amino acid contacts only for the inhibitor moiety distant from the heme macrocycle are shown. Distances are in Angstroms. ( E ) Amino acid residues within 5 Å of bound posaconazole in NfCYP51 (highlighted in bold) are propagated to the CYP51 sequences from the indicated species. Residue labeling is according to NfCYP51. Secondary structure elements on the top are labeled according to the nomenclature introduced elsewhere.[ 47 ] The color scheme is according to the side chains: hydrophilic neutral ( cyan ), aromatic ( purple ), hydrophobic ( green ) and proline ( ochre ). Residue conservation is indicated by the color shades, with pale → bright gradient corresponds to conservation levels. Invariant positions are in brightest shades.
Techniques Used: Binding Assay, Labeling
Figure Legend Snippet: Spectroscopic analysis of recombinant NfCYP51. ( A ) Absolute UV-visible spectra of 3.5 μM purified recombinant NfCYP51: ferric, Fe 3+ ,—solid line, ferrous, Fe 2+ ,—dashed line. Inset: Fe 2+ - Fe 2+ CO difference spectra. ( B) Type I (31-norlanosterol) and type II (posaconazole) difference spectra both added in 500 nM increments to 3.5 μM NfCYP51. ( C ) Binding isotherm of 31-norlanosterol added in 25 nM increments to 0.2 μM NfCYP51 and absorbance difference spectra (Inset). ( D ) Binding isotherms of posaconazole and fluconazole, both added in 50 nM increments to 0.5 μM NfCYP51, show a linear increase in signal up until the equivalence point, after which no further increase in signal was detected.
Techniques Used: Recombinant, Purification, Binding Assay