2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Topoisomerase
  4. PD 0305970

PD 0305970 是一种具有口服活性的细菌 (bacterial) 促旋酶 (gyrase) 和拓扑异构酶 (topoisomerase) 抑制剂。PD 0305970 对革兰氏阳性菌和苛养菌表现出优异的活性，对革兰氏阴性菌的活性则相对温和。PD 0305970 的自发耐药频率较低。PD 0305970 在小鼠链球菌败血症和肺炎球菌肺炎模型中显示出抗菌功效。PD 0305970 可用于细菌感染的研究。

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PD 0305970

PD 0305970 Chemical Structure

CAS No. : 351372-19-5

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PD 0305970 相关抗体

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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

PD 0305970 is an orally active bacterial gyrase and topoisomerase inhibitor. PD 0305970 shows exceptional activity against gram-positive and fastidious organisms and more modest activity against gram-negative species. PD 0305970 shows low spontaneous resistance frequencies. PD 0305970 shows antibacterial efficacy in murine streptococcal sepsis and pneumococcal pneumonia models. PD 0305970 can be used for the research of bacterial infection[1].

体外研究
(In Vitro)

PD 0305970 可强效抑制 1036 株临床细菌分离株的生长，对革兰氏阳性菌和苛养菌表现出优异活性，而对革兰氏阴性菌的活性相对较弱。PD 0305970 可抑制 90% 以上受试菌株的各自最低抑菌浓度 (μg/mL) 范围如下：针对葡萄球菌为 0.125～0.5、链球菌为 0.03～0.06、肠球菌为 0.25～2；针对卡他莫拉菌、流感嗜血杆菌、单核细胞增生李斯特菌、嗜肺军团菌及奈瑟菌属均为 0.25～0.5[1]。
PD 0305970 显示出较低的自发耐药频率[1]。
PD 0305970 (24 h) 对肺炎链球菌 SVI (MIC = 0.008 μg/mL) 和化脓性链球菌 C203 (MIC = 0.008 μg/mL) 表现出快速且持久的杀菌活性[1]。

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

PD 0305970 相关抗体:
体内研究
(In Vivo)

PD 0305970 (0.7-82 mg/kg；口服；单剂量；细菌攻击时给药) 在小鼠脓毒症模型中对多种细菌病原体展现出强大的体内效力，其 PD50 值因感染病原体的不同在 0.7 mg/kg 至 82 mg/kg 之间波动[1]。
PD 0305970 (3.2-4.1 mg/kg；口服；第 1 天每日 1 次，随后 3 天每日 2 次) 对小鼠体内 Levofloxacin (HY-B0330) 敏感型和耐药型肺炎球菌性肺炎均表现出强效的体内药效，其 PD50 值分别为 3.2 mg/kg 和 4.1 mg/kg[1]。

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

Animal Model: CD1 mice (6- to 8-week-old, 18- to 22-g female, bacterial sepsis model via intraperitoneal injection of ~100-fold median lethal doses of bacteria)[1]
Dosage: 0.7-82 mg/kg
Administration: p.o.; single dose; at time of bacterial challenge
Result: Demonstrated a PD50 of 1.9 mg/kg against Methicillin (HY-121544)-susceptible Staphylococcus aureus UC-76.
Demonstrated a PD50 of 2.5 mg/kg against Methicillin-resistant Staphylococcus aureus SA-1417.
Demonstrated a PD50 of 23 mg/kg against ciprofloxacin- and Methicillin-resistant Staphylococcus aureus SA-2017.
Demonstrated a PD50 of 2.7 mg/kg against Streptococcus pneumoniae SVI.
Demonstrated a PD50 of 0.7 mg/kg against Streptococcus pyogenes C203.
Demonstrated a PD50 of 19 mg/kg against Enterococcus faecalis MGH-2.
Demonstrated a PD50 of 82 mg/kg against Escherichia coli Vogel.
分子量

361.41

Formula

C18H24FN5O2
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

PD 0305970 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:

PD 0305970351372-19-5PD0305970PD-0305970BacterialTopoisomerasemurine pneumococcal pneumonia modelstaphylococcal speciesstreptococcipneumococcal speciesmurine streptococcal sepsis modelbacterial DNA gyrase subunit Bgram-positive bacteriafastidious bacteriatopoisomerase IV subunit EStreptococcus pneumoniaeInhibitorinhibitorinhibit

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