Posaconazole

SKU: orb1300976

Description

Posaconazole is a potent small molecule inhibitor of sterol 14α-demethylase, exhibiting an IC50 of 0.25 nM. This antifungal agent is widely used in research to study fungal pathogenesis and treatment, with applications in both in vitro assays and in vivo animal models of infection.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	171228-49-2
MW	700.78
Purity	99.00% (May vary between batches)
Formula	C₃₇H₄₂F₂N₈O₄
SMILES	C([C@@]1(C[C@H](COC2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)N5C(=O)N([C@H]([C@H](C)O)CC)N=C5)CO1)C6=C(F)C=C(F)C=C6)N7C=NC=N7
Target	Antifungal,Parasite
Solubility	Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:245 mg/mL (349.61 mM)

Bioactivity

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Target IC50	C14ɑ demethylase:0.25 nM
In Vivo	Posaconazole exhibits enhanced efficacy against clinically relevant intracellular, non-flagellated parasitic forms. Its minimum inhibitory concentration (MIC) and IC50 are 3 nM and 0.25 nM, respectively. Posaconazole is active against strains of Candida and Aspergillus that are resistant to fluconazole, voriconazole, and amphotericin B, showing superior effectiveness compared to other triazole antifungal agents. It synergizes with amiodarone and disrupts the internal calcium (Ca2+) homeostasis in T. cruzi. Additionally, posaconazole demonstrates a dose-dependent effect on the proliferation of the extracellular (pre-flagellar) stage, with an MIC of 20 nM and an IC50 of 14 nM. Read more...
In Vitro	The bioavailability of Posaconazole is significantly increased by food intake, especially a high-fat diet. When consumed with high-fat and non-fat meals, the systemic exposure to Posaconazole is respectively quadrupled and increased by 2.6 times. Administration of Posaconazole (≥15 mg/kg, b.i.d) can extend the lifespan of mice and reduce tissue burden. Used alone in infected animals, Amiodarone reduces parasitemia and increases the survival rate to 60% at 60 days (compared to 0% in untreated controls), demonstrating this effect. When used in combination, Posaconazole and Amiodarone can delay the progression of parasitemia. This suggests that Posaconazole and Amiodarone may offer an effective, low-side-effect treatment against T. cruzi. When Posaconazole is taken fasting with Boost Plus, there is an increase in drug exposure. Read more...
Cell Research	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 ° Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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POS, Posaconazole, SCH 56592, SCH56592, SCH-56592, inhibit, Inhibitor, Fungal, Antifungal

Quality Guarantee

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Compound Identifiers

PubChem CID

468595 ↗

Key Properties

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No computed properties available.

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Posaconazole (orb1300976)

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Purity:	98.77% (May vary between batches)
CAS Number:	149809-43-8
MW:	449.47
Formula:	C₂₁H₂₁F₂N₃O₄S

CAS Number:	1198769-38-8
MW:	718.79
Formula:	C₃₇H₄₄F₂N₈O₅

CAS Number:	170985-86-1
MW:	790.90
Formula:	C₄₄H₄₈F₂N₈O₄

Purity:	>98% (HPLC)
CAS Number:	171228-49-2
MW:	700.7774
Formula:	C₃₇H₄₂F₂N₈O₄

Posaconazole

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Posaconazole (orb1300976)

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