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Reagents and instruments for immunology, cell biology and molecular biology.

Posaconazole [171228-49-2]

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Cat# HY-17373-10mg

Size : 10mg

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Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.

For research use only. We do not sell to patients.

Posaconazole Chemical Structure

CAS No. : 171228-49-2

This product is a controlled substance and not for sale in your territory.

Based on 8 publication(s) in Google Scholar

Other Forms of Posaconazole:

Posaconazole-d₅ Get quote
Posaconazole-d₄ Get quote
Posaconazole hydrate Get quote
Posaconazole (Standard) Get quote

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Description

Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity.

Cellular Effect

Cell Line	Type	Value	Description	References
3T3	EC₅₀	< 1 nM Compound: 1	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	[PMID: 24120539]
A549	EC₅₀	37 μg/mL Compound: POS	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	[PMID: 28395217]
BEAS-2B	EC₅₀	26 μg/mL Compound: POS	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	[PMID: 28395217]
C3H 10T1/2	IC₅₀	0.14 μM Compound: PSZ	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	[PMID: 27014922]
Caco-2	IC₅₀	1.61 μM Compound: POSACONAZOLE	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	10.21203/rs.3.rs-23951/v1
Caco-2	CC₅₀	14.64 μM Compound: POSACONAZOLE	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	10.21203/rs.3.rs-23951/v1
Hepatocyte	IC₅₀	0.05 μM Compound: Posaconazole	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	[PMID: 24948565]
HUVEC	GI₅₀	1.6 μM Compound: PSZ	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	[PMID: 27014922]
J774	IC₅₀	1.6 μM Compound: Posaconazole	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	[PMID: 27048943]
L6	IC₅₀	> 100 μM Compound: Posa, Noxafil	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 23462713]
L6	IC₅₀	0.0007 μM Compound: Posa, Noxafil	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	[PMID: 23462713]
L6	IC₅₀	0.001 μM Compound: Posaconazole	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	[PMID: 24304150]
Medulloblastoma cell	GI₅₀	1.5 μM Compound: PSZ	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	[PMID: 27014922]
NIH3T3	EC₅₀	0.3 nM Compound: Posaconazole	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	[PMID: 20429511]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

700.78

Formula

C₃₇H₄₂F₂N₈O₄

CAS No.

171228-49-2

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4270 mL	7.1349 mL	14.2698 mL
5 mM	0.2854 mL	1.4270 mL	2.8540 mL
10 mM	0.1427 mL	0.7135 mL	1.4270 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.88 mg/mL (2.68 mM); Clear solution

This protocol yields a clear solution of ≥ 1.88 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.94%

Select Batch:

SDS (393 KB)

COA (247 KB) LCMS (97 KB)

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]

Cell Assay ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

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

Posaconazole Related Classifications

Anti-infection
Fungal Parasite

Posaconazole [171228-49-2]

Cat# HY-17373-10mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

Other Forms of Posaconazole:

View All Parasite Isoform Specific Products:

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Posaconazole Related Classifications

Keywords:

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Posaconazole [171228-49-2]

Cat# HY-17373-10mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

Other Forms of Posaconazole:

View All Parasite Isoform Specific Products:

Posaconazole Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Posaconazole Related Classifications

Keywords:

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