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.
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- 화학식: C22H21NO3
- 분자량:347.41
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보관:
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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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
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.
In Vivo
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.
Chemical Information
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분자량 347.41
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PA36-2 Related Classifications
HY-181404 Related Classifications
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