P163-0892
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.
For research use only. We do not sell to patients.
- CAS No.: 1574576-45-6
- Formula: C19H20N2O3S
- Molecular Weight:356.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
>256 μg/mL
Compound: P163-0892; R-0892
|
Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
|
[PMID: 35922963] |
| Erythrocyte | IC50 |
>256 μg/mL
Compound: P163-0892; R-0892
|
Cytotoxicity against rabbit RBC assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
Cytotoxicity against rabbit RBC assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay
|
[PMID: 35922963] |
| HUVEC | IC50 |
>64 μg/mL
Compound: P163-0892; R-0892
|
Cytotoxicity against human HUVEC cells assessed as inhibition on cell growth incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human HUVEC cells assessed as inhibition on cell growth incubated for 24 hrs by CCK-8 assay
|
[PMID: 35922963] |
In Vitro
P163-0892 (0-32 μg/mL; 48 h) shows antifungal activity with a MIC of 0.25 μg/mL and 0.5 μg/mL against Cryptococcus neoformans and Cryptococcus gattii, respectively[1].
P163-0892 has good aqueous solubility[1].
P163-0892 has no cytotoxicity and no obvious cardiotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wax moth larva infected with C. neoformans H99 or C. gattii WM178[1]
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Dosage:10 mg/kg
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Administration:5 days
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Result:Increased the survival rate of larvae.
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Animal Model:Male Sprague–Dawley rats weighing 200–250 g[1]
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Dosage:2 mg/kg or 5 mg/kg
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Administration:Intravenous or oral administration (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of P163-0892a[1]
route dose (mg/kg) T1/2 (h) Tmax (h) AUC0-inf (h•ng/mL) Cl (mL/h/kg) MRT0-t (h) Vdss (L/kg) BA (%) iv 2 mg/kg 7.61 749 172 2.63 7.12 po 5 mg/kg 15.3 3.17 NR 3.83 NR 0.8
aAbbreviations: iv, intravenous; po, per os; T1/2, half-life elimination in hours; Tmax, time of maximal concentration in hours; AUC, area under the curve; Cl, clearance; MRT, mean residence time; Vdss, volume of distribution at the steady state; BA, bioavailability; NR, not reportable; n = 3.
Chemical Information
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CAS No. 1574576-45-6
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Molecular Weight 356.44
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Formula C19H20N2O3S
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SMILES
O=C(C1=C(O)C2=C(C=CS2)N(CC3=CC=CC=C3)C1=O)NCCCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)