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.
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- CAS No.: 351372-19-5
- Formule: C18H24FN5O2
- Masse moléculaire:361.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
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.
In Vivo
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.
Chemical Information
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CAS No. 351372-19-5
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Masse moléculaire 361.41
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PD 0305970 Related Classifications
HY-182417 Related Classifications
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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