Lascufloxacin
Based on 1 Customer Validation
Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.
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- Purity : 98.04%
- CAS No.: 848416-07-9
- 화학식: C21H24F3N3O4
- 분자량:439.43
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보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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Quinolone |
In Vitro
In the Gram-negative bacteria, Lascufloxacin shows antibacterial activities against Moraxella catarrhalis and β-lactamase-negative ampicillin-susceptible and ampicillin-resistant strains of Haemophilus influenzae, with an MIC90 value of 0.06 μg/mL in all cases. The MIC90 values against Enterobacter spp., Klebsiella pneumoniae, and Acinetobacter spp. are 0.25 μg/mL, 0.25 μg/mL, and 0.5 μg/mL, respectively. Lascufloxacin inhibits E. coli and P. aeruginosa with MIC90s of 0.25 μg/mL and 4 μg/mL, respectively. The MIC50 and MIC90 values of Lascufloxacin against M. pneumoniae are 0.12 μg/mL and 0.25 μg/mL, respectively. Lascufloxacin shows potent activity against macrolide-resistant M. pneumoniae isolates with an MIC90 of 0.12 μg/mL[1].
The MICs of Lascufloxacin against parent S. aureus strains ranged from 0.008 to 0.015 μg/mL, and those against fourth-step parC, gyrA, parC, and gyrA mutant strains are all 2 μg/mL. Lascufloxacin shows incomplete cross-resistance against the mutant strains. The activities of Lascufloxacin against first- and second-step mutant strains of S. pneumoniae are more potent than the activities of other quinolones, and the MICs of Lascufloxacin against gyrA and parC double mutants are 0.25 to 0.5 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 848416-07-9
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Appearance Solid
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분자량 439.43
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화학식 C21H24F3N3O4
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Color White to off-white
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SMILES
O=C(C1=CN(CCF)C2=C(C=C(F)C(N3C[C@H](CNC4CC4)[C@H](F)C3)=C2OC)C1=O)O
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Synonyms
KRP-AM1977
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
In Vitro:
DMSO : 250 mg/mL (568.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
순도&문서
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kishii R, et al. In Vitro Activities and Spectrum of the Novel Fluoroquinolone Lascufloxacin (KRP-AM1977). Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e00120-17. [Content Brief]
[2]. Furuie H, et al. Intrapulmonary Pharmacokinetics of Lascufloxacin in Healthy Adult Volunteers. Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e02169-17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2757 mL | 11.3784 mL | 22.7568 mL | 56.8919 mL |
| 5 mM | 0.4551 mL | 2.2757 mL | 4.5514 mL | 11.3784 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2757 mL | 5.6892 mL | |
| 15 mM | 0.1517 mL | 0.7586 mL | 1.5171 mL | 3.7928 mL | |
| 20 mM | 0.1138 mL | 0.5689 mL | 1.1378 mL | 2.8446 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9103 mL | 2.2757 mL | |
| 30 mM | 0.0759 mL | 0.3793 mL | 0.7586 mL | 1.8964 mL | |
| 40 mM | 0.0569 mL | 0.2845 mL | 0.5689 mL | 1.4223 mL | |
| 50 mM | 0.0455 mL | 0.2276 mL | 0.4551 mL | 1.1378 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3793 mL | 0.9482 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2845 mL | 0.7111 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5689 mL |
Lascufloxacin Related Classifications
HY-16745 Related Classifications
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