2. Anti-infection
  3. Bacterial
  4. Debio 1453

Debio 1453 是一种杀菌性 (bactericidal) FabI 抑制剂，对淋病奈瑟菌 (IC50 = 0.6 nM) 及其耐药菌株具有强效杀菌作用。Debio 1453 通过同时抑制 FabI 和结合不可突变的 NADH 辅因子的作用机制，展现出低耐药性选择倾向，并能有效清除浮游菌和细胞内细菌。Debio 1453 能在小鼠阴道感染模型中清除耐药性淋病奈瑟菌感染。Debio 1453 可用于淋病相关研究。

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Debio 1453

Debio 1453 Chemical Structure

CAS No. : 2422053-29-8

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Debio 1453 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Debio 1453 is a bactericidal FabI inhibitor potent against N. gonorrhoeae (IC50 = 0.6 nM), including drug-resistant strains. Debio 1453 demonstrates a low propensity for resistance selection and is effective in eradicating both planktonic and intracellular bacteria through a mechanism of concurrently inhibiting FabI and engaging the non-mutable NADH cofactor. Debio 1453 clears antibiotic-resistant N. gonorrhoeae infection in a murine vaginal model. Debio 1453 can be used for gonorrhoea research[1].

体外研究
(In Vitro)

Debio 1453 对 2024 株世界卫生组织淋病奈瑟菌参考菌株显示出活性，其中包括对 Ceftriaxone (HY-B0712)、Azithromycin (HY-17506)、Spectinomycin (HY-B0438)、Tetracycline (HY-A0107)和 Ciprofloxacin (HY-B0356) 耐药的菌株，其 MIC 范围为 0.03-0.125 μg/mL[1]。
Debio 1453 对 100 株当代临床分离的淋病奈瑟菌表现出强效的体外活性 (MIC50/MIC90 = 0.06 μg/mL)，MIC 范围为 0.008 至 0.125 μg/mL[1]。
Debio 1453 (0-16 倍 MIC，0-24 小时) 以时间依赖性方式快速杀菌，可有效杀灭对抗生素敏感和广泛耐药 (XDR) 的淋病奈瑟菌[1]。
Debio 1453 (0-8 倍 MIC，0-24 小时) 对体内已存在的对抗生素敏感的淋病奈瑟菌 (ATCC 49226) 和耐药淋病奈瑟菌 (WHO X) 均有效，在 24 小时内即可将每种受试分离株的细菌清除至检测限以下 (分别减少 ≥3.1 log10 CFU/mL 和 ≥2.8 log10 CFU/mL)[1]。
Debio 1453 (4-16 倍 MIC) 在体外对淋病奈瑟菌的耐药突变株的筛选能力较低，从而验证了 FabI 是其作用靶点[1]。
Debio 1453 (0.3-30 μM, 24 小时) 在 HepG2 细胞中未表现出细胞毒性或对细胞活力的负面影响，且在淋巴细胞中无论是否存在大鼠肝脏代谢活化系统，均未显示致染色体断裂或非整倍体毒性[1]。

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

Debio 1453 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: human hepatocytes (HepG2)
Concentration: 0.3, 1, 3, 10, and 30 μM
Incubation Time: 24 h
Result: Showed no cytotoxicity or negative impact on cell viability at all concentrations tested, including the highest concentration of 30 μM.
体内研究
(In Vivo)

Debio 1453 (以 Debio 1453 P 前药形式给药，10-160 mg/kg，口服，每日两次，持续 2 天) 在淋病奈瑟菌阴道感染模型和金黄色葡萄球菌大腿感染两种小鼠模型中均显示出强效抗菌活性[1]。

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

Animal Model: Ovariectomized BALB/c female mice (5-6 weeks) infected intravaginally with N. gonorrhoeae strains[1]
Dosage: 10, 20, 30, 40, 80, and 160 mg/kg (dosed as Debio 1453 P)
Administration: p.o., twice daily for 2 days
Result: Demonstrated efficacy against all tested strains, producing clear dose-response relationships.
Achieved ~3 log10 CFU/mL reductions as compared to the start of treatment (0 h) and eradicated N. gonorrhoeae to the limit of detection by 48 h at multiple dose levels.
Animal Model: Neutropenic female ICR mice infected intravaginally with S. aureus[1]
Dosage: 10, 20, 30, 40, and 80 mg/kg (dosed as Debio 1453 P)
Administration: p.o., twice daily for 2 days
Result: Achieved >1 log10 CFU/mL reductions in thighs at 24 h and >2 log10 CFU reductions at 48 h, displaying efficacy comparable to a supratherapeutic dose of Linezolid (HY-10394).
分子量

420.46

Formula

C23H24N4O4
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

Debio 1453 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Debio 14532422053-29-8Debio1453Debio-1453BacterialFabIN. gonorrhoeaemurine vaginal gonorrhoeaantibiotic-resistantS. aureusInhibitorinhibitorinhibit

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