Name: Posaconazole
Brand: Selleck Chemicals
SKU: S1257
Availability: InStock
Rating: 5 (28 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Dehydrogenase HSP Transferase PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other P450 (e.g. CYP17) Inhibitors	Apigenin Baicalein Avasimibe Naringenin Diosmetin Alizarin Sodium Danshensu Naringin Benzbromarone Orteronel

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human hepatocytes	Function assay			Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method, IC50=0.05 μM	24948565
3T3	Antitrypanosomal assay			Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells, EC50=0.0003μM	19875282
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as accumulation of lanosterol and eburicol precursors at 5 uM after 72 hrs	20385875
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as reduction in episterol content at 5 uM after 72 hrs	20385875
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as reduction in fecosterol content at 5 uM after 72 hrs	20385875
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as accumulation of lanosterol and eburicol precursors at 5 uM after 72 hrs	20385875
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as reduction in episterol content at 5 uM after 72 hrs	20385875
BESM	Function assay	5 uM	72 hrs	Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as reduction in fecosterol content at 5 uM after 72 hrs	20385875
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	20429511
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	20547819
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	20547819
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	20547819
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	23462713
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	24120539
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	24304150
C2C12	Function assay	100 nM	24 hrs	Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as increase in lanosterol level at 100 nM incubated for 24 hrs by GC-MS method	25393646
C2C12	Function assay	100 nM	24 hrs	Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as increase in eburicol level at 100 nM incubated for 24 hrs by GC-MS method	25393646
C2C12	Function assay	100 nM	24 hrs	Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as reduction in episterol level at 100 nM incubated for 24 hrs by GC-MS method	25393646
C2C12	Function assay	100 nM	24 hrs	Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as reduction in fecosterol level at 100 nM incubated for 24 hrs by GC-MS method	25393646
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	27014922
ASZ	Function assay		48 hrs	Inhibition of hedgehog pathway in mouse ASZ cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by qPCR method, IC50=0.54μM	27014922
MERP MB	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse MERP MB cells assessed as cell growth inhibition using methyl-[3H]thymidine after 48 hrs by liquid scintillation spectrophotometry, GI50=1.5μM	27014922
J774	Antileishmanial assay		72 hrs	Antileishmanial activity against Leishmania amazonensis infected in mouse J774 cells after 72 hrs using 2 hrs parasite exposed mouse J774 cells, IC50=1.6μM	27048943
ASZ	Function assay		48 hrs	Inhibition of hedgehog signaling pathway in mouse ASZ cells assessed as decrease in Gli1 mRNA expression after 48 hrs by qRT-PCR analysis, IC50=0.5μM	30529635
Ptch-CKO	Function assay			Inhibition of hedgehog signaling pathway in hedgehog-dependent mouse Ptch-CKO cells assessed as inhibition of cell growth, GI50=1.5μM	30529635
Caco2	Function assay			Substrate activity at P-gp in human Caco2 cells by LC-MS/MS analysis	30529635
Vero	Antiviral assay			Antiviral activity against DENV2 16881 infected in African green monkey Vero cells by qRT-PCR analysis, EC50=4.1μM	31128447
Caco-2	Function assay		48 hrs	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=1.61μM	ChEMBL
Caco-2	Function assay		48 hrs	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=14.64μM	ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (142.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight	700.78	Formula	C₃₇H₄₂F₂N₈O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	171228-49-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SCH 56592, POS			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

Mechanism of Action

Features	Currently the most advanced candidate for the treatment of Chagas disease.
Targets/IC₅₀/Ki	lanosterol 14α-demethylase CYP3A4
In vitro	Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with this compound. It also affects and disrupts Ca²⁺ homeostasis in T. cruzi. This chemical blocks the biosynthesis of ergosterol, which is essential for parasite survival. It 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, this compound is even more potent. It has the minimal inhibitory concentration and IC50 values of 3 nM and 0.25 nM. It 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.
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. Coadministration of this compound and Boost Plus increases drug exposure compared to the administration of this compound alone in the fasted state. Food, particularly meals high in fat content, significantly increases this compound's bioavailability. Systemic exposure to this compound increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively. This compound and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect. At twice-daily doses of ≥15 mg/kg of body weight, this compound prolongs the survival of the mice and reduces tissue burden.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16451055/ [2] https://pubmed.ncbi.nlm.nih.gov/16723559/ [3] https://pubmed.ncbi.nlm.nih.gov/16641468/ [4] https://pubmed.ncbi.nlm.nih.gov/22591838/ [5] https://pubmed.ncbi.nlm.nih.gov/12069997/ [6] https://pubmed.ncbi.nlm.nih.gov/15311563/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin		28383032
Growth inhibition assay	Cell proliferation		28383032

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06282718	Not yet recruiting	Acute Respiratory Tract Infection	European Clinical Research Alliance for Infectious Diseases (ECRAID)\|UMC Utrecht\|University of Oxford\|Universiteit Antwerpen	February 2024	--
NCT06158360	Recruiting	Thyroid Cancer	Ilsan Cha hospital	January 1 2024	--
NCT05845359	Withdrawn	Bariatric Surgery Candidate	Montefiore Medical Center	September 2023	Phase 4
NCT06302842	Active not recruiting	Supportive Care	Istituto Auxologico Italiano	July 1 2023	Not Applicable
NCT05617638	Recruiting	Pain	Hospital Israelita Albert Einstein\|Beneficência Portuguesa de São Paulo	June 27 2023	Not Applicable

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Posaconazole P450 (e.g. CYP17) inhibitor

Chemical Structure

Molecular Weight: 700.78