2. Anti-infection Membrane Transporter/Ion Channel
  3. Fungal P-glycoprotein
  4. PA36-2

PA36-2 是一种 Mdr1 抑制剂和唑类耐药逆转剂，对白色念珠菌 Mdr1 的 IC50 为 1.0 μg/mL，Kd 为 4.209 μM。PA36-2 通过有效抑制 Mdr1 外排泵的活性，阻止了底物被泵出细胞，增强细胞内唑类抗生素的积累，可与 Fluconazole (FLC) (HY-B0101) 等抗真菌剂发挥协同作用。PA36-2 可用于唑类耐药念珠菌病的研究。

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PA36-2

PA36-2 Chemical Structure

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PA36-2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

PA36-2 (0.25 μg/mL; 24 h) 与 FLC 具有强协同作用，可逆转过表达 MDR1 的白色念珠菌菌株 G5 和 SCMPG2A-MRRI (P683S/P683S) 的唑类耐药性，其 FICI <0.5[1]。
PA36-2 (0.5-2 μg/mL; 30 min-6 h) 通过有效抑制 Mdr1 外排泵的活性，阻止了底物 (如Rh123 (HY-D0816) 和 FLC）被泵出白色念珠菌 G5 菌株和酿酒酵母 AD-pdr5-CaMdr1 菌株细胞，从而增加了这些底物在细胞内的积累。
PA36-2 对人阴道上皮细胞 (VK2/E6E7) 和人肝细胞 (HL-7702) 的细胞毒性较低，其 EC50 值＞50 μg/mL[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PA36-2 相关抗体:
体内研究
(In Vivo)

PA36-2 (每只幼虫 0.5 μg; 注射于其右侧末尾前腿处; 单次剂量) 与 FLC 联用在大蜡螟能有效抑制 Mdr1 过表达的白色念珠菌感染，显著提高感染宿主的生存率并清除真菌[1]。
PA36-2 (1 mg/kg; i.p.; 每日一次连续 3 天) 与 FLC 联用在小鼠系统性念珠菌病模型中展现出强效的体内抗真菌活性[1]。

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.
分子量

347.41

Formula

C22H21NO3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PA36-2 相关分类

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  • Do most proteins show cross-species activity?

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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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