1. Cell Cycle/DNA Damage Anti-infection
  2. Topoisomerase Bacterial
  3. 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.

GSK945237

GSK945237 Chemical Structure

CAS No. : 944406-54-6

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Description

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[1].

In Vitro

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.

In Vivo

GSK945237 (50 and 100 mg/kg, i.g., b.i.d. for 2 days starting 1 h post infection) exhibits potent efficacy by reducing the bacterial load in a rat respiratory tract infection model caused by the quinolone-resistant S. pneumoniae TPS3[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats infected by the S. pneumoniae TPS3 (quinolone-resistant)[1]
Dosage: 50 and 100 mg/kg
Administration: i.g., b.i.d. for 2 days starting 1 h post infection
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.
Molecular Weight

451.49

Formula

C24H26FN5O3

CAS No.
SMILES

O=C1N2C3=C([C@H](CN4CCC(NCC5=NN=C(OCCO6)C6=C5)CC4)C2)C(F)=CC=C3C=C1

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GSK945237
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HY-111047
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