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Fig. 1 · Structure
Cat. No.
A10744
CAS No.
171228-49-2
Formula
C37H42F2N8O4
Mol. Weight
700.8

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Posaconazole

Cat. No. A10744 CAS 171228-49-2

CYP3A4 inhibitor

Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14α demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.

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Biological Activity

Target & Activity

Target Activity Value
lanosterol 14α-demethylase

Cellular Effect

Cell Line Activity Value Description Reference
3T3 EC50 < 1 nM Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in 3T3 cells after 7 days by beta-galactosidase assay [PMID: 24120539]
A549 EC50 37 μg/mL 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 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 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 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 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 Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method [PMID: 24948565]
HUVEC GI50 1.6 μM 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 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 Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay [PMID: 23462713]
L6 IC50 0.0007 μM 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 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 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 Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 7 days by alamar blue assay [PMID: 20429511]

14 records · Scroll to view more

In Vitro Studies

In Y strain-infected U2OS cell cultures, Posaconazole yielded an average normalized infection ratio of 7.0 ±6.0%, with incomplete infection reduction in the study using a DMSO negative control. Against A. fumigatus isolate 2, Posaconazole MIC values measured by microbroth dilution were CLSI: 0.031 µg/ml; EUCAST: 0.125 µg/ml. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Incomplete infection reduction in cultured cells

Cell-based study · U2OS cells tissue cultures in 384-well plates were infected with the Y strain [1]

Posaconazole was assessed by compound plating in Y strain-infected U2OS cell cultures, using a DMSO negative control. The average normalized infection ratio was 7.0 ±6.0%; infection was not completely reduced.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Av. Norm. Inf. Ratio (%)average normalized infection ratio 8.0 × 10−8 M, 144 h: 7.0 ±6.0%[1]

Literature-Reported Treatment Conditions

Treatment concentration
8.0 × 10−8 M
Exposure duration
144 h
Method
compound plating
Vehicle
1% DMSO
Co-treatment
Other interventions in this design: Y strain trypomastigotes 2.8 × 103. Compound effect isolated by the comparison: negative (1% DMSO).
Methods and source locations

Compound reported in the paper: Posaconazole

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Time-kill assays (S53); Methods > Compound preparation (S84, S85); Methods > Antiparasitic activity assays (S95); Methods > Time-kill assay (S99, S101); Methods > Data analysis (S106); Figure 3 legend (S120, S122); Table 3 (T3.h1, T3.h2, T3.r10)

Av. Norm. Inf. Ratio (%): Av. Norm. Inf. Ratio (%); comparator: negative (1% DMSO) and positive controls (non-infected cells) — Results > Time-kill assays (S53); Table 3 (T3.h1, T3.h2, T3.r10)

Minimum inhibitory concentrations against Aspergillus fumigatus

Cell-based study · A. fumigatus; isolate 2 [2]

Posaconazole was assessed against A. fumigatus isolate 2 using microbroth dilution. MIC values were CLSI: 0.031 µg/ml; EUCAST: 0.125 µg/ml.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
MIC (µg/ml)MIC CLSI: 0.031 µg/ml; EUCAST: 0.125 µg/ml[2]

Literature-Reported Treatment Conditions

Method
microbroth dilution format
Reported limits
Not stated in the sentences used: dose, schedule, vehicle, control.
Methods and source locations

Compound reported in the paper: Posaconazole

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Strain identification and susceptibility testing (S16); Results > Strain identification and in vitro susceptibility (S82); Table 1 legend (S118); Table 1 (T1.h1, T1.h2, T1.r2)

MIC (µg/ml): MIC (µg/ml) — Table 1 legend (S118); Table 1 (T1.h1, T1.h2, T1.r2)

In Vivo Studies

Immunosuppressed NMRI mice with azole-susceptible A. fumigatus isolate 2 received oral Posaconazole at 20 mg/kg. Posaconazole significantly improved survival when compared to untreated animals. [2]

Survival in immunosuppressed mice with susceptible Aspergillus

Animal study · NMRI mice; immunosuppressed; A. fumigatus isolate 2, with an azole susceptible phenotype [2]

Immunosuppressed NMRI mice with azole-susceptible A. fumigatus isolate 2 received oral Posaconazole at 20 mg/kg. Posaconazole significantly improved survival when compared to untreated animals.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
survivalReported result Posaconazole significantly improved survival[2]

Conditions shared by the study groups

Route
p.o.
Treatment course
once daily on days 1–4 (Monday to Friday) and 7–10 (Monday to Thursday)
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Posaconazole 20 mg/kgglucose i.p. (control mice)Posaconazole significantly improved survival[2]
Posaconazole 20 mg/kg
Model: NMRI mice; immunosuppressed; A. fumigatus isolate 2, with an azole susceptible phenotype
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Posaconazole

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Immunosuppressed haematogenous invasive aspergillosis mouse model (S55); Materials and Methods > In vivo drug efficacy (S59, S60, S62); Results > Development of secondary azole resistance following prolonged antifungal drug exposure (S86)

survival: survival; comparator: glucose i.p. (control mice) — Results > Development of secondary azole resistance following prolonged antifungal drug exposure (S86)

Posaconazole 20 mg/kg · Materials and Methods > In vivo drug efficacy (S62); Results > Development of secondary azole resistance following prolonged antifungal drug exposure (S86)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 171228-49-2
Applications CYP3A4 inhibitor
Formula C37H42F2N8O4
Molecular Weight 700.8
Synonyms Noxafil
SMILES
CC[C@@H]([C@H](C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OC[C@H]5C[C@](OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 90 mg/mL (128.42 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
1% DMSO+30% polyethylene glycol+1% Tween 80

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Moraes CB, Giardini MA, Kim H, et al. Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development. Sci Rep (2014). PMID: 24736467 DOI: 10.1038/srep04703 Source material
  2. [2] Arendrup MC, Mavridou E, Mortensen KL, et al. Development of azole resistance in Aspergillus fumigatus during azole therapy associated with change in virulence. PLoS One (2010). PMID: 20404915 DOI: 10.1371/journal.pone.0010080 Source material

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