2. Metabolic Enzyme/Protease Anti-infection
  3. Dihydrofolate reductase (DHFR) Bacterial
  4. DHFR-IN-26

DHFR-IN-26 是一种大肠杆菌二氢叶酸还原酶 (ecDHFR) 抑制剂，其 IC50 为 0.75 nM。DHFR-IN-26 具有广谱抗菌活性。DHFR-IN-26 干扰叶酸代谢、核苷酸合成以及细菌氨基酸代谢通路。DHFR-IN-26 破坏细菌内膜，抑制生物膜形成，并减弱噬菌体相关过程。DHFR-IN-26 对非癌变细胞的毒性较低。DHFR-IN-26 可用于细菌感染 (包括耐甲氧西林金黄色葡萄球菌 、多重耐药大肠杆菌 、多重耐药铜绿假单胞菌及溶原性细菌) 相关研究。

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DHFR-IN-26

DHFR-IN-26 Chemical Structure

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DHFR-IN-26 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

DHFR-IN-26 is an Escherichia coli dihydrofolate reductase (ecDHFR) inhibitor with an IC50 of 0.75 nM. DHFR-IN-26 exerts broad-spectrum antibacterial activity. DHFR-IN-26 disrupts folate metabolism, nucleotide synthesis, and bacterial amino acid metabolic pathways. DHFR-IN-26 disrupts bacterial inner membranes, inhibited biofilm formation, and attenuated phage-related processes. DHFR-IN-26 shows lower toxicity to non-cancerous cells. DHFR-IN-26 can be used for the research of bacterial infections (including infections caused by methicillin-resistant Staphylococcus aureus, multidrug-resistant Escherichia coli, multidrug-resistant Pseudomonas aeruginosa, and lysogenic bacteria)[1].

体外研究
(In Vitro)

DHFR-IN-26 (compound 4d) (作用时长 24 h) 对革兰氏阳性菌 (包括 MRSA) 和革兰氏阴性菌 (包括 MDR) 菌株展现出广谱抗菌活性，其 MIC 值范围为 0.0625 至 4 μg/mL[1]。
DHFR-IN-26 (0.3-100 μM；作用 24 小时) 对人正常 LO2 细胞的细胞毒性 (IC50 = 124.4 μM) 低于 5-Fluorouracil (HY-90006) (IC50 = 111.31 μM)，而对 Hela 细胞的细胞毒性高于 5-Fluorouracil[1]。
DHFR-IN-26 (4×、8× MIC；于 0 h、30 min、1 h、2 h、4 h、6 h、24 h 取样) 对 金黄色葡萄球菌 (S. aureus) CMCC 25923 和大肠杆菌 (E. coli) CMCC 25922 表现出杀菌效力[1]。
DHFR-IN-26 (用于测定生物膜抑制活性的测试浓度；作用时长 24 h) 可强效抑制 S. aureus 和 E. coli 的生物膜形成，在浓度为 0.5 μg/mL (针对 S. aureus) 和 8 μg/mL (针对 E. coli) 时可实现完全抑制[1]。
DHFR-IN-26 (1×、2×、4×、8×、16× MIC；作用 30 分钟) 可破坏 E. coli CMCC 25922 的内膜通透性，且在 2× MIC 时效果达到峰值[1]。
DHFR-IN-26 (0.5×、1×、2×、4×、8× MIC；作用 6 h) 可破坏 E. coli 细胞膜，进而引发 DNA 和蛋白质的剂量依赖性渗漏[1]。
DHFR-IN-26 (1 μg/mL (溶原菌生长/噬菌体释放)；0、0.5×、1×、2× MIC (黏附)；12 h (溶原菌生长/噬菌体释放)、30 min (黏附)) 可抑制溶原菌生长、阻断子代噬菌体释放，并降低溶原性细菌的宿主细胞黏附能力[1]。

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

DHFR-IN-26 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Human normal LO2 cells, human cancer Hela cells
Concentration: 0.3-100 μM
Incubation Time: 24 h
Result: Exhibited an IC50 of 124.4 μM against LO2 cells and an IC50 of 69.75 μM against Hela cells.
体内研究
(In Vivo)

DHFR-IN-26 (compound 4d) (5 mg/kg、10 mg/kg、20 mg/kg 和 50 mg/kg；腹腔注射；单次给药) 在 BALB/c 小鼠中具有较高的安全性，其 LD50 为 17.39 mg/kg[1]。

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

343.31

Formula

C17H12F3N5
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

DHFR-IN-26 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

DHFR-IN-26Dihydrofolate reductase (DHFR)BacterialEscherichia colimultidrug-resistant pseudomonas aeruginosanucleotide synthesisEscherichia coli dihydrofolate reductasemultidrug-resistant escherichia colilysogenic bacteriagram-positive bacterial strainsecDHFRmethicillin-resistant staphylococcus aureusfolate metabolismInhibitorinhibitorinhibit

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