KRP-AM1977|CAS 848416-07-9|DC Chemicals

Cas No.:	848416-07-9
Chemical Name:	Lascufloxacin
Synonyms:	FILGOTINIB;Lascufloxacin;55MOB566V7;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;7-[(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxoquinoline-3-carboxylic acid;7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidin- 1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo- 1,4-dihydroquinoline-3-carboxyl;Lascufloxacin [INN];7-[(3S,4S)-3-[(Cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic ac
SMILES:	F[C@@H]1CN(C2=C(C=C3C(C(C(=O)O)=CN(CCF)C3=C2OC)=O)F)C[C@@H]1CNC1CC1
Formula:	C₂₁H₂₄F₃N₃O₄
M.Wt:	439.428175926209
Purity:	98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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[1][2].
In Vivo:	A pharmacodynamic study using a mouse thigh infection model indicates that the ratios of the free area under the curve (fAUC) to MIC in plasma required for bacteriostasis, or 1-log or 2-log CFU killing against S. pneumoniae isolates, are 10, 16, and 28, respectively. Lascufloxacin shows significant bacterial killing in the mouse model when emulated the area under the concentration-time curve (AUC) in plasma in dose of 75 mg per day [q.d.]) [2].
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].
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. [2]. Furuie H, et al. Intrapulmonary Pharmacokinetics of Lascufloxacin in Healthy Adult Volunteers. Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e02169-17.

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