Topoisomerase I-IN-22
Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection.
For research use only. We do not sell to patients.
- CAS No.: 3080330-34-0
- Formula: C34H38ClN5O2S
- Molecular Weight:616.22
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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
Biological Activity
Topoisomerase I-IN-22 (Compound 5dl) exhibits potent antibacterial activity against Staphylococcus aureus (ATCC 29213) and 10 clinical MRSA isolates, with an MIC ranging from 0.5 to 2 μg/mL[1].
Topoisomerase I-IN-22 (4-8 × MIC; 0-24 h) exhibits rapid bactericidal activity and rapidly kills S. aureus ATCC 29213 and MRSA-11[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Vss_obs |
|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.747 h | 1.46 L/kg |
Topoisomerase I-IN-22 (6-12 mg/kg; i.p.; administered twice at 12 h intervals) exhibits dose-dependent in vivo anti-MRSA activity in a mouse sepsis model. At the dose of 12 mg/kg, it reduces the liver bacterial load by approximately 2.23 log10 CFU/g and increases the survival rate of mice to 50% in lethal infections[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming (KM) (female, 6−8 weeks old, SPF-grade)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:local administration at abscess site; for 3 doses at 24, 26 and 50 h
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Result:Reduced skin bacterial load by approximately 1.8 log10 CFU/g.
Decreased bacterial survival rate by approximately 96.4%.
Reduced TNF-α levels by approximately 95.2 pg/mL.
Reduced IL-6 levels by approximately 48.2 pg/mL (at 5 mg/kg vs untreated control).
Reduced skin bacterial load by approximately 5.3 log10 CFU/g.
Decreased bacterial survival rate by approximately 97.9%.
Reduced TNF-α levels by approximately 147.3 pg/mL.
Reduced IL-6 levels by approximately 58.1 pg/mL (at 10 mg/kg vs untreated control).
Showed minimal inflammatory cell infiltration in subcutaneous tissue, nearly matching the blank control group (at 10 mg/kg).
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Animal Model:BALB/c (female, 7−8 weeks old, SPF-grade)[1]
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Dosage:6 mg/kg; 12 mg/kg
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Administration:i.p.; two doses 12 hours apart
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Result:Reduced bacterial load in liver by 2.23 log10 CFU/g, in kidneys by 1.83 log10 CFU/g, and in spleen by 1.85 log10 CFU/g (at 12 mg/kg vs untreated control).
Resulted in a 16.7% mouse survival rate in lethal sepsis (at 6 mg/kg).
Resulted in a 50% mouse survival rate in lethal sepsis, matching the efficacy of vancomycin at 12 mg/kg (at 12 mg/kg).
Showed marked improvement in liver, spleen, and kidney tissue damage, with no tubular epithelial cell degeneration/necrosis in kidneys and clear demarcation between red and white pulp in the spleen (at 12 mg/kg).
Chemical Information
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CAS No. 3080330-34-0
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Molecular Weight 616.22
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Formula C34H38ClN5O2S
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SMILES
O=C1C2=C(N=C3N1CCC4=C3N(CCCCSC5=CC=[N+](C=C5)CC(NCCCCC)=O)C6=CC=CC=C46)C=CC=C2.[Cl-]
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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)
Topoisomerase I-IN-22 Related Classifications
HY-182816 Related Classifications
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- Topoisomerase I-IN-22
- 3080330-34-0
- Topoisomerase
- DNA/RNA Synthesis
- Bacterial
- MRSA cell membrane
- S. aureus ATCC 29213
- methicillin-resistant staphylococcus aureus
- mouse skin abscess model
- MRSA DNA Topoisomerase I
- mammalian cells
- mouse sepsis model
- human DNA Topoisomerase I
- intracellular reactive oxygen species
- clinical MRSA isolates
- Inhibitor
- inhibitor
- inhibit