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Posaconazole

Catalog No. T6211   CAS 171228-49-2
Synonyms: SCH 56592, POS

Posaconazole (POS) is a sterol C14ɑ demethylase inhibitor (IC50: 0.25 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Posaconazole Chemical Structure
Posaconazole, CAS 171228-49-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 61.00
10 mg In stock $ 98.00
25 mg In stock $ 178.00
50 mg In stock $ 231.00
100 mg In stock $ 413.00
1 mL * 10 mM (in DMSO) In stock $ 96.00
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Purity: 100%
Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Posaconazole (POS) is a sterol C14ɑ demethylase inhibitor (IC50: 0.25 nM).
Targets&IC50 C14ɑ demethylase:0.25 nM
Kinase Assay In vitro Aβ reduction assays : Human embryonic kidney cells (American Type Culture Collection CRL-1573), transfected with the gene for APP751 (HEK 293) are used for routine Aβ reduction assays. Cells are plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. DAPT are diluted from stock solutions in dimethylsulfoxide (DMSO) to yield a final concentration equal to 0.1% DMSO in media. Cells are pre-treated for 2 hours at 37 °C with DAPT, media are aspirated off and fresh compound solutions applied. After an additional 2-hour treatment period, conditioned media is drawn off and analyzed by a sandwich ELISA (266–3D6) specific for total Aβ. Reduction of Aβ production is measured relative to control cells treated with 0.1% DMSO and expressed as a percentage inhibition. Data from at least six doses in duplicate are fitted to a four-parameter logistical model using XLfit software in order to determine potency. Human and PDAPP mouse neuronal cultures are grown in serum-free media to enhance their neuronal characteristics, and appeared to be greater than 90% neurons after maturation prior to use. Conditioned media to establish baseline Aβ values are collected by adding fresh media to each well and incubated for 24 hours at 37 °C in the absence of DAPT. Cultures are then treated with fresh media containing DAPT at the desired range of concentrations for an additional 24 hours at 37 °C, and conditioned media collected. For the measurement of total Aβ, samples are analyzed with the same ELISA (266–3D6) as used for the HEK 293 cell assays. Analyses of samples for Aβ42 production are performed by a separate ELISA (21F12–3D6) that utilizes a capture antibody specific for the Aβ42 C-terminus. Inhibition of production for both total Aβ and Aβ42 are determined by the difference between the values for the compound treatment and baseline periods.After plotting percentage inhibition versus DAPT concentration, data are analyzed with XLfit software, as above, to determine potency.
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 °
Synonyms SCH 56592, POS
Molecular Weight 700.78
Formula C37H42F2N8O4
CAS No. 171228-49-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (132.7 mM)

TargetMolReferences and Literature

1. Benaim G, et al. J Med Chem. 2006, 49(3), 892-389. 2. Sabatelli F, et al. Antimicrob Agents Chemother. 2006, 50(6), 22009-22015. 3. Sansone-Parsons A, et al. Antimicrob Agents Chemother. 2006, 50(5), 1881-1883. 4. Veiga-Santos P, et al. Int J Antimicrob Agents. 2012, 40, 61-71. 5. Sun QN, et al. Antimicrob Agents Chemother. 2002, 46(7), 2310-2312.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Infection Compound Library Fluorochemical Library Antibiotics Library Anti-Fungal Compound Library Drug-induced Liver Injury (DILI) Compound Library Orally Active Compound Library ReFRAME Related Library Covalent Inhibitor Library Anti-COVID-19 Compound Library Clinical Compound Library

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Keywords

Posaconazole 171228-49-2 Microbiology/Virology Antifungal Inhibitor SCH56592 inhibit SCH 56592 POS SCH-56592 Fungal inhibitor

 

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