PA36-2
PA36-2 is an Mdr1 inhibitor and azole resistance reversal agent, with a IC50 of 1.0 μg/mL and a Kd of 4.209 μM against Candida albicans Mdr1. By effectively inhibiting the activity of the Mdr1 efflux pump, PA36-2 prevents the pumping of substrates out of cells, enhances the intracellular accumulation of azole antibiotics, and exerts a synergistic effect with antifungal agents such as Fluconazole (FLC) (HY-B0101). PA36-2 can be used in the research of azole-resistant candidiasis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C22H21NO3
- 分子量:347.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
PA36-2 (0.25 μg/mL; 24 h) exerts strong synergistic effects with FLC and reverses azole resistance in MDR1-overexpressing Candida albicans strains G5 and SCMPG2A-MRRI (P683S/P683S), with an FICI < 0.5[1].
PA36-2 (0.5-2 μg/mL; 30 min-6 h) prevents the efflux of substrates (e.g., Rh123 (HY-D0816) and FLC) out of Candida albicans strain G5 and Saccharomyces cerevisiae strain AD-pdr5-CaMdr1 by effectively inhibiting the activity of the Mdr1 efflux pump, thereby increasing the intracellular accumulation of these substrates[1].
PA36-2 exhibits low cytotoxicity against human vaginal epithelial cells (VK2/E6E7) and human liver cells (HL-7702), with an EC50 value > 50 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
PA36-2 (1 mg/kg; i.p.; once daily for 3 consecutive days) combined with FLC exhibits potent in vivo antifungal activity in a mouse model of systemic candidiasis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Galleria mellonella (0.28-0.35 g, candidiasis model via injection of Mdr1-overexpressing Candida albicans strain G5)[1]
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Dosage:0.5 μg per larva
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Administration:injection into last right pro-leg; single dose
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Result:Produced minimal effect on larval survival. Resulted in fungal burden significantly higher than in larvae treated with PA36-2 and fluconazole combination. Revealed a large number of fungal cells via periodic acid-Schiff (PAS) staining.
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Animal Model:BALB/c (female, 6-8 weeks old, 18-22 g, disseminated candidiasis model via tail vein injection of Mdr1-overexpressing Candida albicans strain G5)[1]
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Dosage:1 mg/kg
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Administration:i.p.; daily; 3 consecutive days starting on the day of infection
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Result:Produced minimal survival improvements in infected mice. Resulted in kidney fungal burden significantly higher than in mice treated with PA36-2 and fluconazole combination. Revealed extensive filamentous fungal cells in kidneys via periodic acid-Schiff (PAS) staining.
化学情報
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分子量 347.41
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分子式 C22H21NO3
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SMILES
O[C@H](C1=C2C=CC=C1)C[C@H](C32OC4=CC=CC5=CC=CC(O3)=C54)NCC
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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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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)
PA36-2 関連分類
HY-181404 関連分類
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