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Cayman Chemical fluconazole
In vitro evaluation of DB766-azole combinations against intracellular L. donovani . Posaconazole (POS; gray bars), ketoconazole (KTC; horizontal striped bars), or <t>fluconazole</t> (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
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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Average 91 stars, based on 1 article reviews
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fluconazole - by Bioz Stars, 2020-09
91/100 stars

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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

doi: 10.1128/AAC.01129-17

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
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

Structures of DB766, posaconazole, ketoconazole, and fluconazole.
Figure Legend Snippet: Structures of DB766, posaconazole, ketoconazole, and fluconazole.

Techniques Used:

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

doi: 10.1371/journal.pntd.0006104

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.
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

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.
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

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    Cayman Chemical fluconazole
    In vitro evaluation of DB766-azole combinations against intracellular L. donovani . Posaconazole (POS; gray bars), ketoconazole (KTC; horizontal striped bars), or <t>fluconazole</t> (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
    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
    https://www.bioz.com/result/fluconazole/product/Cayman Chemical
    Average 91 stars, based on 1 article reviews
    Price from $9.99 to $1999.99
    fluconazole - by Bioz Stars, 2020-09
    91/100 stars
      Buy from Supplier

    92
    Cayman Chemical fluconazole flc
    In vitro evaluation of DB766-azole combinations against intracellular L. donovani . Posaconazole (POS; gray bars), ketoconazole (KTC; horizontal striped bars), or <t>fluconazole</t> (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
    Fluconazole Flc, supplied by Cayman Chemical, used in various techniques. Bioz Stars score: 92/100, based on 2 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/fluconazole flc/product/Cayman Chemical
    Average 92 stars, based on 2 article reviews
    Price from $9.99 to $1999.99
    fluconazole flc - by Bioz Stars, 2020-09
    92/100 stars
      Buy from Supplier

    Image Search Results


    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

    Journal: Antimicrobial Agents and Chemotherapy

    Article Title: Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations

    doi: 10.1128/AAC.01129-17

    Figure Lengend 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

    Article Snippet: Azoles were obtained from the following sources: ketoconazole was from TCI (Portland, OR), posaconazole was from Carbosynth (San Diego, CA), and fluconazole was from Cayman Chemical (Ann Arbor, MI).

    Techniques: In Vitro, Serial Dilution, Concentration Assay, Inhibition

    Structures of DB766, posaconazole, ketoconazole, and fluconazole.

    Journal: Antimicrobial Agents and Chemotherapy

    Article Title: Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations

    doi: 10.1128/AAC.01129-17

    Figure Lengend Snippet: Structures of DB766, posaconazole, ketoconazole, and fluconazole.

    Article Snippet: Azoles were obtained from the following sources: ketoconazole was from TCI (Portland, OR), posaconazole was from Carbosynth (San Diego, CA), and fluconazole was from Cayman Chemical (Ann Arbor, MI).

    Techniques:

    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.

    Journal: PLoS Neglected Tropical Diseases

    Article Title: CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)

    doi: 10.1371/journal.pntd.0006104

    Figure Lengend 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.

    Article Snippet: [ ] Azole inhibitors were purchased from commercial sources: fluconazole from Cayman Chemical, clotrimazole, miconazole (racemic mix) and voriconazole from Sigma-Aldrich, ketoconazole and itraconazole from Alfa Aesar, voriconazole and isavuconazole from StruChem (China).

    Techniques: Binding Assay, Labeling

    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.

    Journal: PLoS Neglected Tropical Diseases

    Article Title: CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)

    doi: 10.1371/journal.pntd.0006104

    Figure Lengend 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.

    Article Snippet: [ ] Azole inhibitors were purchased from commercial sources: fluconazole from Cayman Chemical, clotrimazole, miconazole (racemic mix) and voriconazole from Sigma-Aldrich, ketoconazole and itraconazole from Alfa Aesar, voriconazole and isavuconazole from StruChem (China).

    Techniques: Recombinant, Purification, Binding Assay