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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- Formule: C22H21NO3
- Masse moléculaire:347.41
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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Masse moléculaire 347.41
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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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)
PA36-2 Related Classifications
HY-181404 Related Classifications
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