Posaconazole
Based on 14 publication(s) in Google Scholar
Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 171228-49-2
- Formula: C37H42F2N8O4
- Molecular Weight:700.78
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Posaconazole
More- Adv Funct Mater. 2025 May 9.
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Clin Chem. 2019 Dec;65(12):1522-1531. [Abstract]
- Microchem J. 2026 Mar 27.
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
- Drug Metab Dispos. 2025 Nov;53(11):100168. [Abstract]
- Microbiol Spectr. 2025 Mar 31:e0318524. [Abstract]
- Mycoses. 2022 Apr;65(4):458-465. [Abstract]
- Am J Cancer Res. 2021 Sep 15;11(9):4528-4540. [Abstract]
- Med Mycol. 2018 Jun 1;56(4):452-457. [Abstract]
- J Mycol Med. 2022 Mar;32(1):101227. [Abstract]
- SSRN. 2026 Mar 7.
- Curr Res Virol Sci. 2022;3:100019. [Abstract]
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Microbiological Assay
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Microbiological Assay
All Parasite Isoforms
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 3T3 | EC50 |
<1 nM
Compound: 1
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in 3T3 cells after 7 days by beta-galactosidase assay
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in 3T3 cells after 7 days by beta-galactosidase assay
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[PMID: 24120539] |
| A549 | EC50 |
37 μg/mL
Compound: POS
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Toxicity in human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin dye based assay
Toxicity in human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin dye based assay
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[PMID: 28395217] |
| BEAS-2B | EC50 |
26 μg/mL
Compound: POS
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Toxicity in human BEAS2B cells assessed as reduction in cell viability incubated for 24 hrs by resazurin dye based assay
Toxicity in human BEAS2B cells assessed as reduction in cell viability incubated for 24 hrs by resazurin dye based assay
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[PMID: 28395217] |
| C3H 10T1/2 | IC50 |
0.14 μM
Compound: PSZ
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Inhibition of hedgehog pathway in mouse C3H10T1/2 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by qPCR method
Inhibition of hedgehog pathway in mouse C3H10T1/2 cells assessed as downregulation of Gli1 mRNA expression after 24 hrs by qPCR method
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[PMID: 27014922] |
| Caco-2 | CC50 |
14.64 μM
Compound: POSACONAZOLE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
1.61 μM
Compound: POSACONAZOLE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
| Hepatocyte | IC50 |
0.05 μM
Compound: Posaconazole
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Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
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[PMID: 24948565] |
| HUVEC | GI50 |
1.6 μM
Compound: PSZ
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Antiproliferative activity against HUVEC assessed as inhibition of VEGF induced cell proliferation after 72 hrs by MTS assay
Antiproliferative activity against HUVEC assessed as inhibition of VEGF induced cell proliferation after 72 hrs by MTS assay
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[PMID: 27014922] |
| J774 | IC50 |
1.6 μM
Compound: Posaconazole
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Antileishmanial activity against Leishmania amazonensis infected in mouse J774 cells after 72 hrs using 2 hrs parasite exposed mouse J774 cells
Antileishmanial activity against Leishmania amazonensis infected in mouse J774 cells after 72 hrs using 2 hrs parasite exposed mouse J774 cells
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[PMID: 27048943] |
| L6 | IC50 |
>100 μM
Compound: Posa, Noxafil
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Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
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[PMID: 23462713] |
| L6 | IC50 |
0.0007 μM
Compound: Posa, Noxafil
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days
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[PMID: 23462713] |
| L6 | IC50 |
0.7 nM
Compound: Posa, Noxafil
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days
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[PMID: 23462713] |
| L6 | IC50 |
0.001 μM
Compound: Posaconazole
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 amastigotes infected in rat L6 cells after 96 hrs by colorimetric method
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 amastigotes infected in rat L6 cells after 96 hrs by colorimetric method
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[PMID: 24304150] |
| Medulloblastoma cell | GI50 |
1.5 μM
Compound: PSZ
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Antiproliferative activity against mouse MERP MB cells assessed as cell growth inhibition using methyl-[3H]thymidine after 48 hrs by liquid scintillation spectrophotometry
Antiproliferative activity against mouse MERP MB cells assessed as cell growth inhibition using methyl-[3H]thymidine after 48 hrs by liquid scintillation spectrophotometry
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[PMID: 27014922] |
| NIH3T3 | EC50 |
0.3 nM
Compound: posaconazole
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells
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[PMID: 19875282] |
| NIH3T3 | EC50 |
0.3 nM
Compound: Posaconazole
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Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay
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[PMID: 20429511] |
| NIH3T3 | CC50 |
>1 μM
Compound: POSA
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Cytotoxicity against mouse 3T3 cells
Cytotoxicity against mouse 3T3 cells
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[PMID: 36111399] |
| Vero | EC50 |
4.1 μM
Compound: Posaconazole
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Antiviral activity against DENV2 16881 infected in African green monkey Vero cells by qRT-PCR analysis
Antiviral activity against DENV2 16881 infected in African green monkey Vero cells by qRT-PCR analysis
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[PMID: 31128447] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 171228-49-2
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Appearance Solid
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Molecular Weight 700.78
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Formula C37H42F2N8O4
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Color White to off-white
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SMILES
FC1=CC=C([C@@]2(CN3C=NC=N3)C[C@H](COC4=CC=C(N5CCN(C6=CC=C(N7C=NN([C@@H](CC)[C@H](C)O)C7=O)C=C6)CC5)C=C4)CO2)C(F)=C1
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Synonyms
SCH 56592
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
Clin Chem
Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]2019 Dec;65(12):1522-1531. PMID: 31578215 -
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Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
BMC Microbiol
In vitro combination effects and mechanisms of Revaprazan with Triazole antifungal drugs on Aspergillus. [Abstract]2025 Nov 5;25(1):715. PMID: 41194018
Posaconazole purchased from MedChemExpress. Usage Cited in: BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
When REV combined with POS, the inhibition zone of ΔAF-MFS32, ΔAF-MFS35 was significantly smaller than that of control group ΔAF-MFS27. REV: Revaprazan (8 µg/ml); POS: posaconazole (8 µg/ml).
Posaconazole purchased from MedChemExpress. Usage Cited in: BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
Rhodamine 6G efflux pump activity. When the wild-type strain WT was used together with Posaconazole (POS, 0. 015–4 µg/mL) in REV and POS, the efflux pump activity was significantly enhanced compared with that of POS alone, which was statistically significant.
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Drug Metab Dispos
Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. [Abstract]2025 Nov;53(11):100168. PMID: 41124962 -
Microbiol Spectr
Synergistic antifungal activity of minocycline as an effective augmenting agent of fluconazole against drug-resistant Candida tropicalis. [Abstract]2025 Mar 31:e0318524. PMID: 40162832 -
Mycoses
COVID-19-associated pulmonary aspergillosis in ICU patients in a German reference centre: Phenotypic and molecular characterisation of Aspergillus fumigatus isolates. [Abstract]2022 Apr;65(4):458-465. PMID: 35138651 -
Am J Cancer Res
Repurposing of posaconazole as a hedgehog/SMO signaling inhibitor for embryonal rhabdomyosarcoma therapy. [Abstract]2021 Sep 15;11(9):4528-4540. PMID: 34659903 -
Med Mycol
2018 Jun 1;56(4):452-457. PMID: 29420769 -
J Mycol Med
In vitro synergistic effect of minocycline combined with antifungals against Cryptococcus neoformans. [Abstract]2022 Mar;32(1):101227. PMID: 34800920 -
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Curr Res Virol Sci
Identification of broad anti-coronavirus chemical agents for repurposing against SARS-CoV-2 and variants of concern. [Abstract]2022;3:100019. PMID: 35072124
Solvent & Solubility
DMSO : 18.75 mg/mL (26.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.88 mg/mL (2.68 mM); Suspended solution
This protocol yields a suspended solution of ≥ 1.88 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.88 mg/mL (2.68 mM); Clear solution
This protocol yields a clear solution of ≥ 1.88 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The epimastigote form of the parasite is cultivated in liver infusion tryptose medium,12 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-1, and drugs are added at a cell density of 0.5−1.0 ×107 epimastigotes mL-1. 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, as described previously. Cells are infected with 10 tissue culture-derived trypomastigotes per cell for 2 h and then washed three times with phosphate-buffered saline (PBS) to remove nonadherent parasites. Fresh medium with and without drugs is added, and the cells are incubated for 96 h with a medium change at 48 h. 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 as described previously. IC50 values are calculated by nonlinear regression, using the program GraFit. Cytoplasmic free Ca2+ concentrations in control and drug-treated extracellular epimastigotes are determined by fluorimetric methods, using Fura-2, again as described previously. Subcellular Ca2+ levels and mitochondrial membrane potentials are monitored on individual Vero cells infected with T. cruzi amastigotes by using time-scan confocal microscopy, as described in detail elsewhere. Briefly, Vero cells heavily infected (72 h) 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 min 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In vivo studies are carried out by using the murine model of acute Chagas' disease in which female NMRI−IVIC mice (20−25 g) are infected with 105 or 103 bloodstream trypomastigotes and drug treatment is started 24 h later. Treatments are given for 30 consecutive days at 20 mg/kg/d for posaconazole (30 doses) and/or at 50 mg/kg every other day for amiodarone (15 doses). Negative controls (i.e. untreated animals) receive only the vehicle, while positive controls are treated with the anti-T. cruzi compound, nifurtimox, at 50 mg/kg/d for 30 days. Survival is followed daily and parasitemia weekly, the latter by direct microscopic examination. Animals are observed for 60 days postinfection, after which time parasitological cures are evaluated by using a combination of hemoculture, xenodiagnosis, and blood PCR tests.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Benaim G, et al. Amiodarone has intrinsic anti-Trypanosoma cruzi activity and acts synergistically with posaconazole. J Med Chem. 2006 Feb 9;49(3):892-9. [Content Brief]
[2]. Sabatelli F, et al. In vitro activities of posaconazole, fluconazole, itraconazole, voriconazole, and amphotericin B against a large collection of clinically important molds and yeasts. Antimicrob Agents Chemother. 2006 Jun;50(6):2009-15. [Content Brief]
[3]. Sansone-Parsons A, et al. Effect of a nutritional supplement on posaconazole pharmacokinetics following oral administration to healthy volunteers. Antimicrob Agents Chemother. 2006 May;50(5):1881-3. [Content Brief]
[4]. Veiga-Santos P, et al. Effects of amiodarone and posaconazole on the growth and ultrastructure of Trypanosoma cruzi. Int J Antimicrob Agents. 2012 Jul;40(1):61-71. [Content Brief]
[5]. Sun QN, et al. In vivo activity of posaconazole against Mucor spp. in an immunosuppressed-mouse model. Antimicrob Agents Chemother. 2002 Jul;46(7):2310-2. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4270 mL | 7.1349 mL | 14.2698 mL | 35.6745 mL |
| 5 mM | 0.2854 mL | 1.4270 mL | 2.8540 mL | 7.1349 mL | |
| 10 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL | 3.5675 mL | |
| 15 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3783 mL | |
| 20 mM | 0.0713 mL | 0.3567 mL | 0.7135 mL | 1.7837 mL | |
| 25 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4270 mL |