Olamufloxacin
Olamufloxacin (HSR-903) is an orally active fluoroquinolone antibacterial agent. Olamufloxacin inhibits DNA supercoiling activity. Olamufloxacin exhibits activity against Gram-positive, Gram-negative, chlamydial, and quinolone-resistant bacterial strains. Olamufloxacin can be used for the research of bacterial infections.
For research use only. We do not sell to patients.
- CAS No.: 167887-97-0
- Formula: C20H23FN4O3
- Molecular Weight:386.43
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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
Olamufloxacin demonstrates potent antimicrobial activity against Gram-positive and Gram-negative clinical bacterial isolates, with MIC50-like MICs ranging from 0.008 mg/L to 0.25 mg/L depending on the strain[1].
Olamufloxacin (18-42 h) potently inhibits growth of gram-positive bacterial clinical isolates including MSSA (MIC90 = 0.78 μg/mL), MRSA (MIC90 = 1.56 μg/mL), PSSP (MIC90 = 0.05 μg/mL), and PRSP (MIC90 = 0.05 μg/mL)[2].
Olamufloxacin (1/4×-2× MIC; 4 h) demonstrates rapid bactericidal activity against S. aureus Smith, E. coli KC-14, and P. aeruginosa E-2[2].
Olamufloxacin potently inhibits E. coli KL-16 DNA gyrase (IC50 = 0.74 μg/mL) but shows weak activity against human placental topoisomerase II (IC50 = 786 μg/mL)[2].
Olamufloxacin (48-72 h) potently inhibits growth of Chlamydia psittaci, Chlamydia trachomatis, and Chlamydia pneumoniae in infected HeLa 229 cells with MICs ranging from 0.016 to 0.063 μg/mL[4].
Olamufloxacin (24 h) potently inhibits growth of clinical Neisseria gonorrhoeae isolates, including those with quinolone resistance-associated alterations in GyrA and ParC[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | AUC0-∞ (Plasma) |
|---|---|---|---|---|---|
| Mice[3] | 50 mg/kg | p.o. | 2.83 h | 1.42 μg/mL | 6.67 μg·h/mL |
Olamufloxacin (50 mg/kg; p.o.; three times daily; 3 days) effectively reduces lung bacterial burden in mice with Penicillin-resistant S. pneumoniae pneumonia[3].
Olamufloxacin (0.625 mg/kg; p.o.; twice daily; 3 days) demonstrates potent activity against H. influenzae respiratory tract infection in ICR mice[3].
Olamufloxacin (5-10 mg/kg; p.o.; twice daily; 5 days) exhibits in vivo efficacy in mice with Chlamydia psittaci-induced pneumonia[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:slc:ICR mice (4-week-old female, 15-19 g) with UTI caused by P. aeruginosa[1]
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Dosage:3.13; 12.5; 50 mg/kg
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Administration:p.o.; twice daily; 3 days
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Result:Resulted in 10/10 survival and a mean log cfu/kidneys count of 1.41 at 50 mg/kg.
Resulted in 9/10 survival and a mean log cfu/kidneys count of 2.72 at 12.5 mg/kg.
Resulted in 6/15 survival and a mean log cfu/kidneys count of 5.82 at 3.13 mg/kg, with no significant reduction versus control.
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Animal Model:CBA/J mice (4-week-old, 15-22 g weight) with pneumonia caused by Penicillin-resistant Streptococcus pneumoniae TUM741[3]
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Dosage:50 mg/kg
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Administration:p.o.; three times daily; 3 days
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Result:Reduced mean lung viable bacterial counts to 3.8 log CFU.
Achieved a 14-day survival rate of 50%.
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Animal Model:ICR mice (4-week-old male, ~20 g weight) with respiratory tract infection caused by Haemophilus influenzae TMS8[3]
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Dosage:0.625 mg/kg
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Administration:p.o.; twice daily; 3 days
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Result:Significantly reduced viable bacterial counts in the lower respiratory tract at all time points post-drug administration.
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Animal Model:ICR mice (5-week-old male) with pneumonia caused by Chlamydia psittaci[4]
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Dosage:5; 10 mg/kg
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Administration:p.o.; twice daily; 5 days
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Result:Achieved a 100% survival rate at day 14 post-infection.
Showed significantly higher or longer survival rates.
Chemical Information
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CAS No. 167887-97-0
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Molecular Weight 386.43
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Formula C20H23FN4O3
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SMILES
N[C@H]1C2(CN(C1)C=3C(C)=C4N(C=C(C(O)=O)C(=O)C4=C(N)C3F)C5CC5)CC2
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Synonyms
HSR-903 free base
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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
[1]. Yoshizumi S, et al. The in vivo activity of olamufloxacin (HSR-903) in systemic and urinary tract infections in mice. J Antimicrob Chemother. 2001;48(1):137-140. [Content Brief]
[2]. Takahashi Y, et al. In vitro activity of HSR-903, a new quinolone. Antimicrob Agents Chemother. 1997;41(6):1326-1330. [Content Brief]
[3]. Yoshizumi S, et al. In vivo activity of HSR-903, a new fluoroquinolone, against respiratory pathogens. Antimicrob Agents Chemother. 1998;42(4):785-788. [Content Brief]
[4]. Niki Y, et al. In vitro and in vivo antichlamydial activities of HSR-903, a new fluoroquinolone antibiotic. Antimicrob Agents Chemother. 1997;41(4):857-859. [Content Brief]
[5]. Deguchi T, et al. In-vitro antimicrobial activity of HSR-903, a new fluoroquinolone, against clinical isolates of Neisseria gonorrhoeae with quinolone resistance-associated alterations in GyrA and ParC. J Antimicrob Chemother. 1997;40(3):437-439. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Olamufloxacin Related Classifications
HY-W683763 Related Classifications
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