P163-0892
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1574576-45-6
- Formule: C19H20N2O3S
- Masse moléculaire:356.44
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
Cellular Effect
|
Cell Line
|
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.
-
Animal Model:Wax moth larva infected with C. neoformans H99 or C. gattii WM178[1]
-
Dosage:10 mg/kg
-
Administration:5 days
-
Result:Increased the survival rate of larvae.
-
Animal Model:Male Sprague–Dawley rats weighing 200–250 g[1]
-
Dosage:2 mg/kg or 5 mg/kg
-
Administration:Intravenous or oral administration (Pharmacokinetic Analysis)
-
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
-
CAS No. 1574576-45-6
-
Masse moléculaire 356.44
-
Formule C19H20N2O3S
-
SMILES
O=C(C1=C(O)C2=C(C=CS2)N(CC3=CC=CC=C3)C1=O)NCCCC
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)