KPI-10

• CAS: 888032-58-4
• Catalog Number: ACM888032584
• Category: Others
• Molecular Weight: 461.45
• Molecular Formula: C22H22F3N5O3
• Description: KPI-10, also known as WQ3810, is a new compound currently being studied for its efficacy in the treatment of infections caused by multidrug-resistant bacteria. WQ-3810 demonstrated high potent activity against the antimicrobial-resistant pathogens tested. WQ-3810 (MIC(90)=4 mg/L and 0.06 mg/L, respectively) was also more active than ciprofloxacin (64 mg/L and 2 mg/L) and levofloxacin (32 mg/L and 2 mg/L). Furthermore, WQ-3810 was the most potent among the fluoroquinolones tested against meticillin-resistant Staphylococcus aureus (MRSA) and Neisseria gonorrhoeae, including FQR isolates.
• Synonyms: KPI-10; KPI10; KPI 10; WQ3810; WQ-3810; WQ 3810
• IUPAC Name: 1-(6-Amino-3,5-difluoropyridin-2-yl)-6-fluoro-7-(3-(isopropylamino)azetidin-1-yl)-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
• Canonical SMILES: O=C(C1=CN(C2=NC(N)=C(F)C=C2F)C3=C(C=C(F)C(N4CC(NC(C)C)C4)=C3C)C1=O)O
• InChI: InChI=1S/C22H22F3N5O3/c1-9(2)27-11-6-29(7-11)18-10(3)17-12(4-14(18)23)19(31)13(22(32)33)8-30(17)21-16(25)5-15(24)20(26)28-21/h4-5,8-9,11,27H,6-7H2,1-3H3,(H2,26,28)(H,32,33)
• InChI Key: MJMVUQNNSOBCGF-UHFFFAOYSA-N
• Solubility: To be determined
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: WQ3810 is an orally active fluoroquinolone, with potent antibacterial activities.
• Drug Formulation: To be determined
• Elemental Analysis: C, 57.26; H, 4.81; F, 12.35; N, 15.18; O, 10.40
• Exact Mass: 461.1675
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: In vitro antimycobacterial activity of WQ-3810 was evaluated against recombinant Mtb var. bovis Bacille Calmette-Guérin strains in which gyrase-coding genes were replaced with Mtb variants containing resistance-conferring mutations. WQ-3810 showed a higher inhibitory activity than levofloxacin against most recombinant DNA gyrases with FQ-resistance mutations. Furthermore, WQ-3810 showed inhibition even against a DNA gyrase variant harboring a G88C mutation which is thought to confer the highest resistance against FQs in clinical Mtb isolates. Since FQs and ethambutol have been used in multi-drug therapy for tuberculosis, WQ-3810 might represent a new, potent anti-tuberculosis drug that can be effective even against FQ-resistant Mtb strains.; Reference: Tuberculosis (Edinb). 2020 Jan;120:101891. https://pubmed.ncbi.nlm.nih.gov/31778929/
• In Vivo Activity: TBD
• Shipping: 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.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).