MedKoo Cat#: 598423 | Name: Lascufloxacin HCl

Description:

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

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

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

Theoretical Analysis

MedKoo Cat#: 598423

Name: Lascufloxacin HCl

CAS#: 1433857-09-0 (HCl)

Chemical Formula: C21H25ClF3N3O4

Exact Mass:

Molecular Weight: 475.89

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 currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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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

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
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.