2. Anti-infection Cell Cycle/DNA Damage
  3. Antibiotic Bacterial Topoisomerase DNA/RNA Synthesis
  4. GC-072

GC-072 是一种口服有效的 4-氧代喹啉抗生素 (antibiotic)，选择性地抑制细菌 DNA 回旋酶 (bacterial DNA gyrase) 和拓扑异构酶 IV (Topo IV) 酶。GC-072 不抑制人拓扑异构酶 I 和 II。 GC-072 对多种细菌菌株，包括革兰氏阳性菌、革兰氏阴性菌和耐药菌，均表现出强效抗菌活性。GC-072 对类鼻疽伯克霍尔德菌 (Burkholderia pseudomallei) 也显示出细胞外和细胞内的杀菌活性。在暴露于致死性吸入性类鼻疽伯克霍尔德菌感染模型的小鼠中，GC-072 可剂量依赖性地提高小鼠存活率。GC-072 可用于研究类鼻疽病。

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GC-072

GC-072 Chemical Structure

CAS No. : 1371629-36-5

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GC-072 相关抗体

Top Publications Citing Use of Products

查看 Antibiotic 亚型特异性产品:

查看所有亚型
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis[1].

IC50 & Target[1]

DNA Gyrase

2 μM (IC50, S. aureus)

TOPO IV

4-30 μM (IC50, S. aureus)

DNA Gyrase

0.18-1.5 μM (IC50, E.coli)

TOPO IV

4.22-8.45 μM (IC50, E.coli)

体外研究
(In Vitro)

GC-072 (0.25 μg/mL，2.5 μg/mL；0、1、5、24 小时) 能以快速的时间和剂量依赖性方式有效抑制小鼠巨噬细胞内类鼻疽伯克霍尔德菌的生长，在两种浓度下 24 小时后均未检测到活菌[1]。
GC-072 可抑制大肠杆菌和沙门氏菌。 GC-072 对大肠杆菌 DNA 回旋酶和拓扑异构酶 IV 均表现出良好的活性。针对金黄色葡萄球菌 DNA 回旋酶、大肠杆菌 DNA 回旋酶、金黄色葡萄球菌拓扑异构酶 IV 和大肠杆菌拓扑异构酶 IV 的 IC50 值分别为 2 μM、0.18-1.50 μM、4-30 μM 和 4.22-8.45 μM[1]。
GC-072 对类鼻疽伯克霍尔德菌也表现出良好的活性，其 MIC90 为 0.25 μg/mL，范围为 ≤0.008 至 1 μg/mL[1]。
GC-072 对 B. anthracis、Y. pestis、F. tularensis 和 B. mallei 等细菌的 MIC90 值分别为 0.002 μg/mL、0.015 μg/mL、≤0.0005 μg/mL 和 0.12 μg/mL[1]。
GC-072 对所测试的耐药类鼻疽伯克霍尔德菌菌株 (即对 Ceftazidime (HY-B0593)、Clavulanate (HY-A0256A) 和 Trimethoprim (HY-B0510) 耐药的菌株) 具有完全活性[1]。

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

GC-072 相关抗体:
体内研究
(In Vivo)

GC-072 (1-30 mg/kg；口服 (灌胃) ；q8h (每天三次)；14 天) 和 GC-072 (37.5-150 mg/kg；口服 (灌胃) ；q8h；14 天) 可提高类鼻疽肺炎模型模型中的生存率 (通过气溶胶挑战感染 B. pseudomallei 菌株 1026b)[1]。

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

Animal Model: BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: oral (gavage); 1, 3, 10, 30 mg/kg; q8h; 14 days
Result: When treatment was initiated 8 h postchallenge, 0%, 0%, 70%, and 90% survival was observed in mice administered 1, 3, 10, and 30 mg/kg, respectively.
When treatment was initiated 16 h postchallenge, 50% and 100% survival was observed in the 10 and 30 mg/kg groups, respectively.
Animal Model: BALB/c (Female, 6 to 8 weeks, 19.75 g) (infected with B. pseudomallei strain 1026b via aerosol challenge)[1]
Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration: oral (gavage); 37.5, 75, 150 mg/kg; q8h; 14 days
Result: When initiated 8 h postexposure, mice in the 37.5-, 75-, and 150-mg/kg treatment groups demonstrated 90%, 90%, and 80% survival, respectively.
In the 24-h treatment initiation groups, overall survival was low. However, each dose provided a significant survival advantage compared to vehicle control.
分子量

370.35

Formula

C20H16F2N2O3
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

GC-072 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:

GC-0721371629-36-5GC072GC 072AntibioticBacterialTopoisomeraseDNA/RNA Synthesisbacterial topoisomerasesreduced development of resistancefirst-lineoral treatmentdrug-resistant strainsmelioidosisbactericidallethal inhalational models4-oxoquinolizine antibioticoral administrationpotentextra- and intracellularlyselective inhibitory activityrapid killingdose-dependent survivalintragastricallyInhibitorinhibitorinhibit

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