PD 0305970
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 351372-19-5
- 分子式: C18H24FN5O2
- 分子量:361.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Topoisomerase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
体外実験
PD 0305970 potently inhibits growth of 1036 clinical bacterial isolates, showing exceptional activity against gram-positive and fastidious organisms and more modest activity against gram-negative species. The respective MICs (μg/mL) for PD 0305970 capable of inhibiting >90% of bacterial strains tested ranged from 0.125 to 0.5 versus staphylococci, 0.03 to 0.06 versus streptococci, 0.25 to 2 versus enterococci, and 0.25 to 0.5 versus Moraxella catarrhalis, Haemophilus influenzae, Listeria monocytogenes, Legionella pneumophila, and Neisseria spp[1].
PD 0305970 shows low spontaneous resistance frequencies[1].
PD 0305970 (24 h) demonstrates rapid and sustained bactericidal activity against Streptococcus pneumoniae SVI (MIC = 0.008 μg/mL) and Streptococcus pyogenes C203 (MIC = 0.008 μg/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
PD 0305970 (3.2-4.1 mg/kg; p.o.; once daily for 1 day, twice daily for 3 days) shows potent in vivo efficacy against both Levofloxacin (HY-B0330)-susceptible and resistant pneumococcal pneumonia in mice, with PD50 values of 3.2 mg/kg and 4.1 mg/kg respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:0.7-82 mg/kg
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Administration:p.o.; single dose; at time of bacterial challenge
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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.
化学情報
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CAS 番号 351372-19-5
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分子量 361.41
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分子式 C18H24FN5O2
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SMILES
CC1=C2N(C3CC3)C(N(C(C2=CC(F)=C1N4C[C@](CC4)([H])[C@@H](N)C)=O)N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Huband MD, et al. In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups. Antimicrob Agents Chemother. 2007;51(4):1191-1201. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PD 0305970 関連分類
HY-182417 関連分類
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Keywords
- PD 0305970
- 351372-19-5
- PD0305970
- PD-0305970
- Bacterial
- Topoisomerase
- murine pneumococcal pneumonia model
- staphylococcal species
- streptococci
- pneumococcal species
- murine streptococcal sepsis model
- bacterial DNA gyrase subunit B
- gram-positive bacteria
- fastidious bacteria
- topoisomerase IV subunit E
- Streptococcus pneumoniae
- Inhibitor
- inhibitor
- inhibit