Lascufloxacin - CAS 848416-07-9
Catalog number: 848416-07-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H24F3N3O4
Molecular Weight:
439.43
COA:
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Targets:
Antibacterial
Description:
Lascufloxacin is an antibacterial drug candidate. Phase-III clinical trials in Respiratory tract infections and in Community-acquired pneumonia in Japan were on-going.
Purity:
98%
Appearance:
Powder
Synonyms:
KRP-AM1977; 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin- 1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo- 1,4-dihydroquinoline-3-carboxylic acid
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
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Application:
Community-acquired pneumonia; Otorhinolaryngological infections; Respiratory tract infections
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
ZFIOCUITTUUVPV-MEDUHNTESA-N
InChI:
1S/C21H24F3N3O4/c1-31-20-17-13(19(28)14(21(29)30)9-26(17)5-4-22)6-15(23)18(20)27-8-11(16(24)10-27)7-25-12-2-3-12/h6,9,11-12,16,25H,2-5,7-8,10H2,1H3,(H,29,30)/t11-,16+/m0/s1
Canonical SMILES:
COc1c(N2C[C@@H](F)[C@@H](CNC3CC3)C2)c(F)cc4C(=O)C(=CN(CCF)c14)C(=O)O
Current Developer:
Originator Kyorin
1.Activities and Spectrum of the Novel Fluoroquinolone Lascufloxacin (KRP-AM1977).
Kishii R;Yamaguchi Y;Takei M Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e00120-17. doi: 10.1128/AAC.00120-17. Print 2017 Jun.
Lascufloxacin exhibited a broad spectrum of activity against various clinical isolates. Furthermore, lascufloxacin showed the most potent activity against Gram-positive bacteria among the quinolones tested and incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin had potent inhibitory activity against both wild-type and mutated target enzymes. These results suggest that lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.
2.Activity of Lascufloxacin against Streptococcus pneumoniae with Mutations in the Quinolone Resistance-Determining Regions.
Murata M;Kosai K;Yamauchi S;Sasaki D;Kaku N;Uno N;Morinaga Y;Hasegawa H;Miyazaki T;Izumikawa K;Mukae H;Yanagihara K Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e01971-17. doi: 10.1128/AAC.01971-17. Print 2018 Apr.
Lascufloxacin showed potent activity against ;Streptococcus pneumoniae; with a GyrA or ParC mutation (first-step mutant). The frequency of selecting resistant strains tended to be lower for lascufloxacin than for levofloxacin and garenoxacin after drug exposure in first-step mutants but was similar in the comparison between lascufloxacin and moxifloxacin. The increase in MIC was smaller for lascufloxacin than for levofloxacin, garenoxacin, and moxifloxacin when clinical strains with only ParC mutations were exposed to the corresponding drug.
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