产品
编 号：F745881
分子式：C19H20N2O3S
分子量：356.44
分子式：C19H20N2O3S
分子量：356.44
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CAS No: 1574576-45-6
产品详情
生物活性：
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.
体内研究：
P163-0892 (10 mg/kg; 5 days) significantly extends the survival of larvae infected with either C. neoformans or C. gattii.Animal Model:Wax moth larva infected with C. neoformans H99 or C. gattii WM178
Dosage:10 mg/kg
Administration:5 days
Result:Increased the survival rate of larvae.
Animal Model:Male Sprague–Dawley rats weighing 200–250 g
Dosage:2 mg/kg or 5 mg/kg
Administration:Intravenous or oral administration (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of P163-0892aroutedose (mg/kg) T1/2 (h) Tmax (h) AUC0-inf (h?ng/mL) Cl (mL/h/kg) MRT0-t (h) Vdss (L/kg) BA (%)
iv2 mg/kg7.617491722.637.12
po5 mg/kg15.33.17NR3.83NR0.8
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.
体外研究：
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.P163-0892 has good aqueous solubility.P163-0892 has no cytotoxicity and no obvious cardiotoxicity.
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.
体内研究：
P163-0892 (10 mg/kg; 5 days) significantly extends the survival of larvae infected with either C. neoformans or C. gattii.Animal Model:Wax moth larva infected with C. neoformans H99 or C. gattii WM178
Dosage:10 mg/kg
Administration:5 days
Result:Increased the survival rate of larvae.
Animal Model:Male Sprague–Dawley rats weighing 200–250 g
Dosage:2 mg/kg or 5 mg/kg
Administration:Intravenous or oral administration (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of P163-0892aroutedose (mg/kg) T1/2 (h) Tmax (h) AUC0-inf (h?ng/mL) Cl (mL/h/kg) MRT0-t (h) Vdss (L/kg) BA (%)
iv2 mg/kg7.617491722.637.12
po5 mg/kg15.33.17NR3.83NR0.8
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.
体外研究：
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.P163-0892 has good aqueous solubility.P163-0892 has no cytotoxicity and no obvious cardiotoxicity.
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