2. Anti-infection
  3. Fungal
  4. Antifungal agent 151

Antifungal agent 151 是一种 Prp8 内含肽抑制剂，可抑制 Prp8 内含肽的自我剪接过程，阻止 Prp8 蛋白的成熟。Antifungal agent 151 对新型隐球菌 (Cryptococcus neoformans) 和格特隐球菌 (Cryptococcus gattii) 具有体外抗真菌活性。Antifungal agent 151 可用于隐球菌肺炎的相关研究。

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Antifungal agent 151

Antifungal agent 151 Chemical Structure

CAS No. : 3097563-43-1

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Antifungal agent 151 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

Antifungal agent 151 is a Prp8 intein inhibitor that inhibits the self-splicing process of the Prp8 intein, preventing maturation of the Prp8 protein. Antifungal agent 151 exerts in vitro antifungal activity against Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent 151 can be used for the research of cryptococcus pneumonia[1].

体外研究
(In Vitro)

Antifungal agent 151 (compound B5)(1–64 μg/mL；48 h) 可强效抑制新生隐球菌 H99、新型隐球菌 R265、氟康唑耐药的新生隐球菌 (菌株 313) 以及新生隐球菌临床分离株的生长，其 MIC 值范围为 0.5 至 2 μg/mL[1]。
Antifungal agent 151 (compound B5)(8.0 μg/mL；直至真菌消除) 对 C. neoformans H99 表现出快速、浓度依赖性的杀菌活性，可在两小时内彻底消除真菌 [1]。
Antifungal agent 151 (compound B5)(2.0 μg/mL；2 h) 诱导新型隐球菌 H99 的转录组重编程，并抑制内含子的正常剪接，导致氧化应激、DNA 损伤应答以及代谢基因表达的改变 [1]。
Antifungal agent 151 (compound B5) 通过氢键以及与 Cys1[1] 之间有利于共价相互作用的距离，结合到 Prp8 内含肽活性位点。
Antifungal agent 151 (compound B5) 对 LO2 细胞的 IC50 值为 14.99 μg/mL，对 A549 细胞的 IC50 值为 10.31 μg/mL。抗真菌剂 151 对 C. neoformans 的 MIC 值较低，使其治疗指数高于 6G-318S[1]。
Antifungal agent 151 (compound B5)(64 μg/mL) 在 64 μg/mL 浓度下表现出良好的血液相容性，溶血率仅为 3.2%[1]。

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

Antifungal agent 151 相关抗体:
体内研究
(In Vivo)

Antifungal agent 151 (compound B5) (10 mg/kg; i.p.; 每日给药；连续 7 天) 可有效降低新型隐球菌 (C. neoformans) 肺炎小鼠模型的真菌载量与病理损伤，且生物安全性良好 [1]。

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

Animal Model: BALB/c (female, 6-8 weeks old, intranasally inoculated with C. neoformans H99)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; 7 days
Result: Significantly reduced pulmonary fungal burden; suppressed fungal invasion in lung tissues; reduced focal lymphocyte infiltration; preserved alveolar structural integrity compared to saline-treated controls.
分子量

377.41

Formula

C16H12FN3O3S2
CAS 号
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

Antifungal agent 151 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Antifungal agent 1513097563-43-1Antifungal agent151Antifungal agent-151FungalCryptococcus neoformansPrp8 inteinLO2 cellsself-splicing processCryptococcus gattiicryptococcus pneumoniaC. neoformans H99C. gattii R265fluconazole-resistant C. neoformansPrp8 proteinInhibitorinhibitorinhibit

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