IMP-2380
IMP-2380 is a NorA inhibitor that binds to the outward-open conformation of Staphylococcus aureus NorA. IMP-2380 enhances the activity of Ciprofloxacin against Methicillin-resistant (HY-121544) and Methicillin-sensitive Staphylococcus aureus. IMP-2380 inhibits Ciprofloxacin-induced SOS response and reduces prophage induction. IMP-2380 reduces bacterial burden in a mouse MRSA infection model in combination with Ciprofloxacin. IMP-2380 can be used for research on Methicillin-resistant Staphylococcus aureus (MRSA) infection.
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- CAS No.: 3088774-28-8
- Formule: C21H16ClN3O2S
- Masse moléculaire:409.89
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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
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- Pureté et documentation
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Activité biologique
Description
In Vitro
IMP-2380 (20 min) inhibits NorA-mediated EtBr efflux in S. aureus with an IC50 of 19 nM[1].
IMP-2380 (1 µM; 30 min) increases intracellular Ciprofloxacin accumulation in wild-type S. aureus[1].
IMP-2380 (1 µM; 6 h) enhances the killing effect of Ciprofloxacin against WT S. aureus by up to 10,000-fold[1].
IMP-2380 (30 µM; 6 h) inhibits Ciprofloxacin-induced prophage activation in S. aureus RN451[1].
IMP-2380 (1 µM; 72 h) completely blocks the emergence of spontaneous Ciprofloxacin tolerance in S. aureus SH1000[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female; 6-8 weeks; Envigo; n = 5 per group)[1]
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Dosage:IMP-2380 30 mg/kg; ciprofloxacin 30 mg/kg
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Administration:i.p.; single dose at 2 h after infection
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Result:Produced no significant decrease in bacterial burden compared with vehicle.
Caused a 100-fold reduction in CFU count, with infections in 3 of 5 animals below the limit of detection of the assay combined with Ciprofloxacin.
Chemical Information
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CAS No. 3088774-28-8
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Masse moléculaire 409.89
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Formule C21H16ClN3O2S
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SMILES
OC(C/C(C1=NC2=CC=CC=C2S1)=C\C3=CN(C)N=C3C4=CC=C(Cl)C=C4)=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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IMP-2380 Related Classifications
HY-189704 Related Classifications
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