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
439.44
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.
| 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: 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.
1. Kuo SC, Wang YC, Tan MC, Huang WC, Shiau YR, Wang HY, Lai JF, Huang IW, Lauderdale TL. In vitro activity of imipenem/relebactam, meropenem/vaborbactam, ceftazidime/avibactam, cefepime/zidebactam and other novel antibiotics against imipenem-non-susceptible Gram-negative bacilli from Taiwan. J Antimicrob Chemother. 2021 May 6:dkab141. doi: 10.1093/jac/dkab141. Epub ahead of print. PMID: 33956969.
2.
