Lascufloxacin HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 598423

CAS#: 1433857-09-0 (HCl)

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 HCl
CAS# 1433857-09-0 (HCl)
Instruction

Theoretical Analysis

MedKoo Cat#: 598423
Name: Lascufloxacin HCl
CAS#: 1433857-09-0 (HCl)
Chemical Formula: C21H25ClF3N3O4
Exact Mass: 0.00
Molecular Weight: 475.890
Elemental Analysis: C, 53.00; H, 5.30; Cl, 7.45; F, 11.98; N, 8.83; O, 13.45

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 848416-07-9 (free base)   1433857-09-0 (HCl)    

Synonym: Lascufloxacin hydrochloride; Lascufloxacin HCl; 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 hydrochloride

InChi Key: YQHZQIJEMFMUGH-DFIJPDEKSA-N

InChi Code: InChI=1S/C21H24F3N3O4.ClH/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);1H/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.[H]Cl

Appearance: 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

Shelf Life: >3 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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 475.89 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: 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.

2: 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.

3: 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.