P163-0892
P163-0892 is a potent and selective antifungal agent against Cryptococcus species. P163-0892 is predicted to show medium BBB penetration.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1574576-45-6
- 分子式: C19H20N2O3S
- 分子量:356.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 1574576-45-6
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分子量 356.44
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)