1. Anti-infection Cell Cycle/DNA Damage
  2. Bacterial DNA/RNA Synthesis
  3. Antibacterial agent 338

Antibacterial agent 338 (Compound 65) 是一种抗菌 (Antibacterial) 剂、GyrB 抑制剂,对大肠杆菌 GyrBIC50 为 12.60 nM。Antibacterial agent 338 可结合大肠杆菌 GyrB 的 ATP 结合域,从而抑制 GyrB 的 ATP 酶活性。Antibacterial agent 338 对多重耐试剂革兰氏阴性菌具有广谱抗菌活性。Antibacterial agent 338 可降低中性粒细胞减少小鼠大腿感染模型中的细菌载量。Antibacterial agent 338 可用于鲍曼不动杆菌感染的研究。

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Antibacterial agent 338

Antibacterial agent 338 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from *E. coli*. Antibacterial agent 338 binds to the ATP-binding domain of *E. coli* GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of *Acinetobacter baumannii* infection[1].

体外研究
(In Vitro)

Antibacterial agent 338 (0.038-10000 nM; 60 min) 可强效抑制大肠杆菌 (E. coli) DNA GyrB ATP 酶活性,其 IC50 为 12.60 nM[1]
Antibacterial agent 338 (0.03-64 μg/mL; 18-20 h) 对多重耐试剂革兰氏阴性菌具有广谱抗菌活性,其中对多重耐试剂鲍曼不动杆菌 Aba-2024-D2-018 的 MIC 为 0.5 μg/mL[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t AUC0-∞ MRT0-∞ T1/2 CL_obs Vss_obs
Rat[1] 5 mg/kg i.v. 2057 ng/mL 961 ng·h/mL 971 ng·h/mL 2.12 h 2.66 h 87.2 mL/min/kg 11.1 L/kg
Mice[1] 20 mg/kg i.v. 35600 ng/mL 16164 16169 0.95 h 0.78 h 20.8 mL/min/kg 1.20 L/kg
体内研究
(In Vivo)

Antibacterial agent 338 (10-20 mg/kg;静脉注射;单次,一日两次) 在中性粒细胞减少小鼠体内对多重耐药鲍曼不动杆菌表现出剂量依赖性的体内效果[1]

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

Animal Model: ICR (half male and half female, 18-22 g, neutropenic via cyclophosphamide injection)[1]
Dosage: 10 mg/kg; 20 mg/kg; 20 mg/kg (two doses 6 hours apart)
Administration: i.v.; single dose; two doses 6 hours apart
Result: Achieved a bacterial burden reduction comparable to positive controls (levofloxacin and compound 9) at 20 mg/kg.
Produced a 2.65-log10 CFU/g reduction in bacterial burden.
Produced a 4.57-log10 CFU/g reduction, corresponding to >99.99% bacterial eradication, with bacterial burden reduced to pretreatment levels.
分子量

489.55

Formula

C25H28FN9O

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
  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
Antibacterial agent 338
目录号:
HY-182936
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