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AdipoGen Life Sciences
Merafloxacin
100
CHF
CHF 100.00
In stock
AG-CR1-3756-M0055 mgCHF 100.00
AG-CR1-3756-M02525 mgCHF 400.00
| Product Details | |
|---|---|
| Synonyms | CI-934; PD 114843; 1-Ethyl-7-(3-((ethylamino)methyl)-1-pyrrolidinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H23F2N3O3 |
| MW | 379.4 |
| CAS | 91188-00-0 |
| Purity Chemicals | ≥98% (NMR) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO. |
| Identity | Determined by 1H-NMR |
| InChi Key | BAYYCLWCHFVRLV-UHFFFAOYSA-N |
| Smiles | O=C1C2=CC(F)=C(N3CCC(CNCC)C3)C(F)=C2N(CC)C=C1C(O)=O |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Merafloxacin is a fluoroquinolone broad-spectrum antibacterial compound. It is an inhibitor of bacterial DNA gyrase and Type II DNA topoisomerase. It demonstrated excellent activity against Gram-positive organisms and less potent activity against Gram-negative bacteria.
- Merafloxacin is a programmed -1 ribosomal frameshifting (-1 PRF) inhibitor of SARS-CoV-2. Frameshift inhibition by merafloxacin is robust to mutations within the pseudoknot region and is similarly effective on -1 PRF of other betacoronaviruses and blocks SARS-CoV-2 replication in Vero E6 cells. The compound reduced viral levels in infected African green monkey VeroE6 cells in a concentration-dependent manner. Merafloxacin showed no cellular toxicity and resulted in a 3 to 4 orders of magnitude reduction of SARS-CoV-2 titer, with IC50 of 4.3 μΜ. This compound provides a starting point for high-throughput screening for frameshifting inhibitors as a viable target for therapeutic intervention against SARS-CoV-2.
Product References
- In vitro activity of CI-934, a quinolone carboxylic acid active against gram-positive and -negative bacteria: M.A. Cohen, et al.; Antimicrob. Agents Chemother. 28, 766 (1985)
- Discrepancy between the antibacterial activities and the inhibitory effects on Micrococcus luteus DNA gyrase of 13 quinolones: K.P. Fu, et al.; Chemotherapy 32, 494 (1986)
- In vitro activity of CI-934 and other antimicrobial agents against gram-positive and gram-negative bacteria: R.P. Smith, et al.; Clin. Ther. 9, 106 (1986)
- In vitro assessment of CI-934-a new quinolone derivative: R. Finch, et al.; Chemioterapia 5, 368 (1986)
- Inhibitory effects of quinolones on DNA gyrase of Escherichia coli and topoisomerase II of fetal calf thymus: K. Hoshino, et al.; Antimicrob. Agents Chemother. 33, 1816 (1989)
- Restriction of SARS-CoV-2 Replication by Targeting Programmed -1 Ribosomal Frameshifting In Vitro: Y. Sun, et al.; Preprint (2020)
- Programmed −1 Ribosomal Frameshifting in coronaviruses: A therapeutic target: J.A. Kelly, et al.; Virology 554, 75 (2021)
- Structural basis of ribosomal frameshifting during translation of the SARS-CoV-2 RNA genome: P.R. Bhatt, et al.; Science (Epub ahead of print) (2021)