2. Anti-infection Membrane Transporter/Ion Channel
  3. Fungal P-glycoprotein
  4. 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.

For research use only. We do not sell to patients.

PA36-2

PA36-2 Chemical Structure

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PA36-2 Related Antibodies

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Description

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[1].

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.

PA36-2 Related Antibodies
In Vivo

PA36-2 (0.5 μg per larva; injected into the right proleg; single dose) combined with FLC effectively inhibits Candida albicans infections with Mdr1 overexpression in Galleria mellonella, significantly improves the survival rate of infected hosts, and eliminates the fungi[1].
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.

Animal Model: Galleria mellonella (0.28-0.35 g, candidiasis model via injection of Mdr1-overexpressing Candida albicans strain G5)[1]
Dosage: 0.5 μg per larva
Administration: injection into last right pro-leg; single dose
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.
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]
Dosage: 1 mg/kg
Administration: i.p.; daily; 3 consecutive days starting on the day of infection
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.
Molecular Weight

347.41

Formula

C22H21NO3
SMILES

O[C@H](C1=C2C=CC=C1)C[C@H](C32OC4=CC=CC5=CC=CC(O3)=C54)NCC
Shipping

Room temperature in continental US; may vary elsewhere.
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PA36-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PA36-2FungalP-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Galleria mellonellafluconazoleCandida albicansnormal human hepatocytesMdr1VK2/E6E7immortalized human vaginal epithelial cellsHL-7702azole resistanceSaccharomyces cerevisiaeInhibitorinhibitorinhibit

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