Merafloxacin

CHF 90.00
In stock
AG-CR1-3756-M0055 mgCHF 90.00
AG-CR1-3756-M02525 mgCHF 360.00
More Information
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
  • 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
  1. 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)
  2. 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)
  3. 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)
  4. In vitro assessment of CI-934-a new quinolone derivative: R. Finch, et al.; Chemioterapia 5, 368 (1986)
  5. 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)
  6. Restriction of SARS-CoV-2 Replication by Targeting Programmed -1 Ribosomal Frameshifting In Vitro: Y. Sun, et al.; Preprint (2020)
  7. Programmed −1 Ribosomal Frameshifting in coronaviruses: A therapeutic target: J.A. Kelly, et al.; Virology 554, 75 (2021)
  8. 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)
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