Posaconazole (SCH 56592)

For research use only.

Catalog No.S1257

18 publications

Posaconazole (SCH 56592) Chemical Structure

CAS No. 171228-49-2

Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

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10mM (1mL in DMSO) EUR 383 In stock
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Selleck's Posaconazole (SCH 56592) has been cited by 18 publications

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  • Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.

    Eur J Pharm Sci, 2016, 91:190-195. . Posaconazole (SCH 56592) purchased from Selleck.

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Biological Activity

Description Posaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
Features Currently the most advanced candidate for the treatment of Chagas disease.
Targets
lanosterol 14α-demethylase [1]
()
CYP3A4 [6]
In vitro

Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with Posaconazole. Posaconazole also affects and disrupts Ca2+ homeostasis in T. cruzi. Posaconazole blocks the biosynthesis of ergosterol, which is essential for parasite survival. Posaconazole has a clear, dose-dependent effect on proliferation of the epimastigote (extracellular) stages, with a minimal inhibitory concentration of 20 nM and an IC50 of 14 nM. Against the clinically relevant intracellular amastigote form of the parasite, Posaconazole is even more potent. Posaconazole has the minimal inhibitory concentration and IC50 values of 3 nM and 0.25 nM. [1] Posaconazole is active against isolates of Candida and Aspergillus spp. that exhibit resistance to Fluconazole, Voriconazole, and Amphotericin B and is much more active than the other triazoles against zygomycetes. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Caco2 NGfGeFlHfW6ldHnvckBie3OjeR?= NUTCelExW3Wkc4TyZZRmKGGldHn2bZR6KGG2IGCt[5AhcW5iaIXtZY4hS2Glb{KgZ4VtdHNiYomgUGMuVVNxTWOgZY5idHm|aYO= MojDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm2N|UoRjNyNUK5OlM2RC:jPh?=
Vero M3nMNGFvfGm4aYLhcEBie3OjeR?= MUPBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDESW5XOiBzNki4NUBqdm[nY4Tl[EBqdiCDZoLpZ4FvKGe{ZXXuJI1wdmuneTDW[ZJwKGOnbHzzJIJ6KHGUVD3QR3Ih[W6jbInzbZMtKEWFNUC9OE4y|ryP M2raOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMUK4OFQ4Lz5|MUGyPFQ1PzxxYU6=
Caco-2 NVPTdnRsTnWwY4Tpc44h[XO|YYm= Ml3ZOFghcHK| MoPHSIV1\XKvaX7heIlwdiCxZjDJR|UxKH[jbIXld{Bnd3JiaX7obYJqfGmxbjDv[kBUSVKVLVPvWk0zKGmwZIXj[YQh[3m2b4TvfIlkcXS7IH;mJGNi[29vMjDj[YxteyCjZoTldkA1QCCqb4Xyd{BjgSCqaXfoJINwdnSnboSgbY1i\2mwZzygTWM2OD1zLk[x{txO MoLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVM6Py9pPlPoSW1DVDxxYU6=
Caco-2 NXXQcZRqTnWwY4Tpc44h[XO|YYm= NH[zcJk1QCCqcoO= MkTzWI95cWOrdImgZYdicW6|dDDDZYNwNTJiY3XscJMh\GW2ZYLtbY5m\CCjdDC0PEBpd3W{czDifUBqdnS{YXPlcIx2dGG{IFHUVEBkd26lZX70doF1cW:wIIXzbY5oKHSqZTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG|c3H5MEBESzVyPUG0MlY1|ryP MmP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVM6Py9pPlPoSW1DVDxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell proliferation ; 

PubMed: 28383032     


The effect of tivozanib on cell viability was estimated by MTT assay.

28383032
Western blot
Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin ; 

PubMed: 28383032     


Protein lysates from tivozanib-treated cells were subjected to Western blotting and probed with the indicated antibodies. β-actin was used as the loading control. The concentrations of tivozanib were 5, 10 and 20 μM. The blots are representative of three independent experiments with similar outcomes. 

28383032
In vivo Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia. [1] Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively. [3] Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect. [4] At twice-daily doses of ≥15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden. [5]

Protocol

Cell Research:

[1]

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  • Cell lines: Epimastigote form of T. cruzi amastigotes
  • Concentrations: 0 nM -4 nM
  • Incubation Time: 96 hours
  • Method:

    The epimastigote form of the parasite is cultivated in liver infusion tryptose medium, supplemented with 10% new born calf serum at 28 °C with strong (120 rpm) agitation. Cultures are initiated at a cell density of 2 × 106 epimastigotes/mL, and Posaconazole is added at a cell density of 0.5−1.0 × 107 epimastigotes/mL. Cell densities are measured by using an electronic particle counter as well as by direct counting with a hemocytometer. Cell viability is followed by Trypan blue exclusion, using light microscopy. Amastigotes are cultured in Vero cells maintained in minimal essential medium supplemented with 1% fetal calf serum in a humidified atmosphere (95% air−5% CO2) at 37 °C. Cells are infected with 10 tissue culture-derived trypomastigotes per cell for 2 hours and then washed three times with phosphate-buffered saline (PBS) to remove nonadherent parasites. Fresh medium with and without Posaconazole is added, and the cells are incubated for 96 hours with a medium change at 48 hours. The percent of infected cells and the numbers of parasites per cell are determined directly using light microscopy, and a statistical analysis of the results is carried out. IC50 values are calculated by nonlinear regression, using the program GraFit. Fractional inhibitory concentrations (FIC) are calculated. Cytoplasmic free Ca2+ concentrations in control and drug-treated extracellular epimastigotes are determined by fluorimetric methods using Fura-2. Subcellular Ca2+ levels and mitochondrial membrane potentials are monitored on individual Vero cells infected with T. cruzi amastigotes by using time-scan confocal microscopy. Briefly, Vero cells heavily infected (72 hours) with T. cruzi amastigotes are plated onto 22 × 40 mm glass coverslips (0.15 mm thickness) and incubated simultaneously with 10 μM cell-permeant Rhod-2 and 10 μg/mL Rhodamine-123 for 50 minutes at 37 °C in culture medium and then washed and incubated with Ringer's solution, with or without amiodarone. Under the conditions used fluorescence of Rhod-2 comes mainly from intracellular Ca2+-rich compartments, like mitochondria, since its low affinity for Ca2+ limits its fluorescence in the Ca2+-poor cytoplasm of the Vero cells or amastigotes. Rhodamine-123 is a mitochondrion-specific cationic dye, which distributes across the inner mitochondrial membranes strictly according to their membrane potential.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female NMRI−IVIC mice with acute Chagas
  • Dosages: 20 mg/kg/d
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (142.69 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 700.78
Formula

C37H42F2N8O4

CAS No. 171228-49-2
Storage powder
in solvent
Synonyms N/A
Smiles CCC(C(C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5CC(OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04825275 Not yet recruiting Drug: Posaconazole Pill Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult Milton S. Hershey Medical Center May 2021 Early Phase 1
NCT04725942 Not yet recruiting Drug: Oral Posaconazole tablets Pulmonary Fungal Infection Institute of Hematology & Blood Diseases Hospital|Shanxi Bethune Hospital|The Second Hospital of Hebei Medical University|Tianjin Medical University Cancer Institute and Hospital January 2021 --
NCT03717623 Recruiting Drug: Posaconazole pharmacokinetics Posaconazole|Pharmacokinetics|Invasive Candidiases|Invasive Aspergillosis|Invasive Mycosis|Fungal Infection|Prophylaxis Melbourne Health|Merck Sharp & Dohme Corp. August 1 2019 Phase 4
NCT03796533 Unknown status Drug: Posaconazole Leukemia Myeloid Acute Hospices Civils de Lyon February 2019 Not Applicable
NCT04194086 Recruiting Drug: posaconazole oral suspensions Leukemia Acute Zhujiang Hospital|Guangdong Provincial People''s Hospital November 1 2018 Phase 1|Phase 2

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID