Lascufloxacin
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MedKoo CAT#: 319549

CAS#: 848416-07-9 (free base)

Description: Lascufloxacin, also known as KRP-AM-1977, is a potent antibacterial drug candidate. Lascufloxacin showed a broad spectrum of activity against various clinical isolates. Especially, lascufloxacin showed the most potent activity against gram-positive bacteria among the quinolones tested. Furthermore, lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant strains. Enzymatic analysis indicated that lascufloxacin showed potent inhibitory activity against both wild-type and mutated target enzymes. Lascufloxacin may be useful in treating infections caused by various pathogens, including quinolone-resistant strains.


Chemical Structure

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Lascufloxacin
CAS# 848416-07-9 (free base)

Theoretical Analysis

MedKoo Cat#: 319549
Name: Lascufloxacin
CAS#: 848416-07-9 (free base)
Chemical Formula: C21H24F3N3O4
Exact Mass: 439.1719
Molecular Weight: 439.4352
Elemental Analysis: C, 57.40; H, 5.51; F, 12.97; N, 9.56; O, 14.56

Price and Availability

Size Price Availability Quantity
5.0mg USD 250.0 Same day
10.0mg USD 450.0 Same day
25.0mg USD 650.0 Same day
50.0mg USD 1050.0 Same day
100.0mg USD 1750.0 Same day
200.0mg USD 3150.0 Same day
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Related CAS #: 848416-07-9 (free base)   1433857-09-0 (HCl)    

Synonym: KRP-AM1977; KRP-AM-1977; KRP-AM 1977; KRP-AM1977X; KRP-AM1977Y; Lascufloxacin

IUPAC/Chemical Name: 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

InChi Key: ZFIOCUITTUUVPV-MEDUHNTESA-N

InChi Code: 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

SMILES Code: O=C(C1=CN(CCF)C2=C(C=C(F)C(N3C[C@H](CNC4CC4)[C@H](F)C3)=C2OC)C1=O)O

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 439.4352 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Ohya K, Takano J, Manita S. In Vitro Mechanistic Study of the Distribution of Lascufloxacin into Epithelial Lining Fluid. Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02208-18. doi: 10.1128/AAC.02208-18. Print 2019 Apr. PubMed PMID: 30718243; PubMed Central PMCID: PMC6437485.

2: Yamagishi Y, Matsukawa Y, Suematsu H, Mikamo H. In vitro activity of lascufloxacin, a novel fluoroquinolone antibacterial agent, against various clinical isolates of anaerobes and Streptococcus anginosus group. Anaerobe. 2018 Dec;54:61-64. doi: 10.1016/j.anaerobe.2018.08.002. Epub 2018 Aug 13. PubMed PMID: 30114441.

3: Murata M, Kosai K, Yamauchi S, Sasaki D, Kaku N, Uno N, Morinaga Y, Hasegawa H, Miyazaki T, Izumikawa K, Mukae H, Yanagihara K. In Vitro Activity of Lascufloxacin against Streptococcus pneumoniae with Mutations in the Quinolone Resistance-Determining Regions. Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e01971-17. doi: 10.1128/AAC.01971-17. Print 2018 Apr. PubMed PMID: 29439959; PubMed Central PMCID: PMC5913943.

4: Furuie H, Tanioka S, Shimizu K, Manita S, Nishimura M, Yoshida H. Intrapulmonary Pharmacokinetics of Lascufloxacin in Healthy Adult Volunteers. Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e02169-17. doi: 10.1128/AAC.02169-17. Print 2018 Apr. PubMed PMID: 29339391; PubMed Central PMCID: PMC5913947.

5: Kishii R, Yamaguchi Y, Takei M. In Vitro Activities and Spectrum of the Novel Fluoroquinolone Lascufloxacin (KRP-AM1977). Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e00120-17. doi: 10.1128/AAC.00120-17. Print 2017 Jun. PubMed PMID: 28320717; PubMed Central PMCID: PMC5444182.