Posaconazole (SCH 56592) - 10mM in DMSO, high purity , CAS No.171228-49-2(DMSO)

Item Number
P409129
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P409129-1ml
1ml
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$1,042.90

CYP3 Selective Inhibitors | Activators

Basic Description

Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsPosaconazole (SCH56592) is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life o
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Product Description

Information

Posaconazole (SCH56592) is an inhibitor primarily ofCYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor ofsterol C14ɑ demethylaseinhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 1
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. 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.

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 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. Posaconazole 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, Posaconazole prolongs the survival of the mice and reduces tissue burden.
Cell Data

cell lines:

Concentrations:0 nM -4 nM

Incubation Time:96 hours

Powder Purity:≥99%

Associated Targets(Human)

CYP3A4 Tclin Cytochrome P450 3A4 (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP11B2 Tchem Cytochrome P450 11B2, mitochondrial (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP11B1 Tclin Cytochrome P450 11B1, mitochondrial (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CYP17A1 Tclin Steroid 17-alpha-hydroxylase/17,20 lyase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES CCC(C(C)O)N1N=CN(C1=O)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(OCC5COC(C5)(C[N]6C=NC=N6)C7=CC=C(F)C=C7F)C=C4
Molecular Weight 700.78

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 57 mg/mL (200.48 mM); Water: 57 mg/mL (200.48 mM); Ethanol: 57 mg/mL (200.48 mM);

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