GSK945237
GSK945237 is a potent and orally active bacterial type IIA topoisomerases inhibitor. GSK945237 shows broad-spectrum activity against Gram-positive and Gram-negative bacteria (IC50 of 0.034 μg/mL against H. influenzae DNA gyrase). GSK945237 demonstrates good in vivo efficacy in a rat respiratory tract infection model. GSK945237 can be used for anti-infection research.
For research use only. We do not sell to patients.
- CAS No.: 944406-54-6
- Formula: C24H26FN5O3
- Molecular Weight:451.49
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
GSK945237 (18-24 h) exhibits antibacterial activity against H. influenzae, S. aureus, and S. pneumoniae with MICs of 1, 0.06, and 0.25 μg/mL, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLblood | Vss | T1/2β | Cmax | AUC |
|---|---|---|---|---|---|---|---|
| Dog[1] | 3 mg/kg | i.v. | 11.9 mL/min/kg | 6.1 L/kg | 8.8 h | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | / | 1.07 μg/mL | 6.05 μg·h/mL |
| Monkey[1] | 3 mg/kg | i.v. | 22.6 mL/min/kg | 8.2 L/kg | 7.6 h | / | / |
| Monkey[1] | 5 mg/kg | p.o. | / | / | / | 0.21 μg/mL | 1.19 μg·h/mL |
| Rat[1] | 3 mg/kg | i.v. | 60.8 mL/min/kg | 7.2 L/kg | 1.9 h | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | / | / | 0.04 μg/mL | 0.29 μg·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats infected by the S. pneumoniae TPS3 (quinolone-resistant)[1]
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Dosage:50 and 100 mg/kg
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Administration:i.g., b.i.d. for 2 days starting 1 h post infection
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Result:Showed excellent efficacy at 50 and 100 mg/kg, with bacterial numbers reduced below the limit of detection in 3/5 and 5/5 animals, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 944406-54-6
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Molecular Weight 451.49
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Formula C24H26FN5O3
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SMILES
O=C1N2C3=C([C@H](CN4CCC(NCC5=NN=C(OCCO6)C6=C5)CC4)C2)C(F)=CC=C3C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK945237 Related Classifications
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