AM-8722
AM-8722 is an orally active inhibitor of bacterial DNA gyrase and topoisomerase IV. AM-8722 inhibits bacterial DNA synthesis and exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative pathogens. AM-8722 can be used for research on bacterial septicemia and bacterial infections.
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: 2230715-40-7
- 分子式: C27H30ClN5O5
- 分子量:540.01
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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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Help & FAQs
生物活性
製品説明
体外実験
AM-8722 is a potent inhibitor of bacterial DNA gyrase and topoisomerase IV from S. aureus and E. coli, with IC50s of 0.83 μM and 0.14 μM for DNA gyrase, respectively, and is selective against human topoisomerase II[1].
AM-8722 exhibits potent broad-spectrum antibacterial activity against various Gram-positive and Gram-negative organisms, including resistant strains[1].
The antibacterial activity of AM-8722 against S. aureus RN4220 is unaffected by the presence of excess DNA or human serum, with an MIC of 0.125 μg/mL[1].
AM-8722 displays potent in vitro activity against a broad panel of clinical isolates, including Staphylococcus, Acinetobacter, H. influenzae, and M. catarrhalis[1].
AM-8722.HCl exhibits potent and rapid bactericidal activity against S. aureus ATCC 29213 at concentrations of 1 μg/mL and above, with no regrowth at 16× MIC or higher[1].
AM-8722 (compound 6) (0.031-8 μg/mL) shows broad-spectrum antibacterial activity with MIC values of 0.031 μg/mL against Staphylococcus aureus Smith, 0.5 μg/mL against Streptococcus pneumoniae IID553, 2 μg/mL against Enterococcus faecium VanA (VRE), 2 μg/mL against Escherichia coli ATCC 25922, 0.25 μg/mL against Acinetobacter baumannii IID876, and 8 μg/mL against Pseudomonas aeruginosa PAO1[2].
AM-8722 exhibits high apparent permeability across MDCKII monolayers with a Papp of 23.6 × 10−6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
AM-8722 (3.2-50 mg/kg; p.o.; single administration; 1 h post-inoculation) exhibits an ED50 of 20.6 mg/kg in a mouse MSSA disseminated infection model, and its efficacy level is consistent with the 21%-27% oral bioavailability of the drug in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (female, immunocompetent, intraperitoneal inoculation with methicillin-susceptible Staphylococcus aureus strain Smith)[1]
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Dosage:3.2-50 mg/kg (i.v.); 3.2-50 mg/kg (p.o.)
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Administration:i.v.; single dose; 1 h post-inoculation
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Result:Achieved an ED50 of 2.1 mg/kg intravenously.
Achieved 1-, 2-, and 3-log reductions (ED90, ED99, and ED99.9) in bacterial burden at 6.3, 11.5, and 17.0 mg/kg intravenously, respectively.
Achieved ED50, ED90, ED99, and ED99.9 of 20.6, 31.6, 42.7, and 52.8 mg/kg orally, respectively.
化学情報
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CAS 番号 2230715-40-7
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分子量 540.01
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分子式 C27H30ClN5O5
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SMILES
O=C1C=CC2=C(N1CCO)C(CCC34OCC(CC3)(CC4)NCC5=NC(N6)=C(C=C5)OCC6=O)=C(Cl)C=N2
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AM-8722 関連分類
HY-187725 関連分類
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