1. Metabolic Enzyme/Protease Anti-infection
  2. Dihydrofolate reductase (DHFR) Bacterial
  3. DHFR-IN-24

DHFR-IN-24 是一种苯并噻唑衍生物,属于二氢叶酸还原酶 (DHFR) 抑制剂。DHFR-IN-24 对革兰氏阳性菌和革兰氏阴性菌均具有固有的抗菌活性。DHFR-IN-24 可将 DHFR 抑制与光动力疗法 (PDT) 协同作用,增强对多重耐药病原体的抗菌活性。

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DHFR-IN-24

DHFR-IN-24 Chemical Structure

CAS No. : 1088704-78-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DHFR-IN-24, a benzothiazole derivative, is a dihydrofolate reductase (DHFR) inhibitor. DHFR-IN-24 has intrinsic antibacterial activity against both Gram-positive and Gram-negative strains. DHFR-IN-24 synergistically combines DHFR inhibition with photodynamic therapy (PDT) for enhanced antibacterial activity against multidrug-resistant pathogens[1].

体外研究
(In Vitro)

DHFR-IN-24 (compound 12) 可抑制耐甲氧西林金黄色葡萄球菌 (MRSA) ATCC 33591、金黄色葡萄球菌 (S. aureus) ATCC 25923、表皮葡萄球菌 (S. epidermidis) CICC 10436、鲍曼不动杆菌 (A. baumannii) Bio 34235、鲍曼不动杆菌 Bio 53272、大肠杆菌 (E. coli) ATCC 25922 和肺炎克雷伯菌 (K. pneumoniae) CICC 21611,其最小抑菌浓度 (MIC) 值分别为 0.5 μg/mL、0.5 μg/mL、2 μg/mL、16 μg/mL、16 μg/mL、4 μg/mL 和 8 μg/mL[1]
DHFR-IN-24 的光动力激活通过在 MRSA 中高效生成活性氧 (ROS),使其抗菌效力增强高达 64 倍[1]
DHFR-IN-24 具有固有的抗菌活性,并且在光动力激活后抗菌活性显著增强[1]
DHFR-IN-24 对革兰氏阳性菌和革兰氏阴性菌均表现出显著的时间和浓度依赖性抗菌作用[1]
DHFR-IN-24 对耐甲氧西林金黄色葡萄球菌 (MRSA) 和鲍曼不动杆菌 (A. baumannii) 具有强效的光增强抗生物膜活性[1]
DHFR-IN-24 对人胚肾细胞 (HEK293T) 和宫颈癌细胞 (HeLa) 没有明显的细胞毒性[1]

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

体内研究
(In Vivo)

DHFR-IN-24 (compound 12) (0.5 mg/mL;外用;14 天) 在可见光激活下可改善全层切取创面的伤口闭合,并根除 Balb/c 中感染的 MRSA 细菌,而仅使用 DHFR-IN-24 的组愈合效果中等,优于 Vancomycin (HY-B0671) 组,但仍逊于光动力疗法组[1]

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

Animal Model: Balb/c (Male, 6-8 weeks, 180-220 g) were subsequently inoculated with 10μL of MRSA suspension[1].
Dosage: 0.5 mg/mLwith lightexposure
Administration: Topical; 14 days
Result: At the experimental end point (day 14), the photodynamic therapy group achieved near-complete wound healing with complete absence of inflammatory signs.
分子量

504.45

Formula

C22H21IN2S2

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
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  • 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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DHFR-IN-24
目录号:
HY-179415
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