yingweiwo

Prulifloxacin

Alias: Prulifloxacin;NM441; Pruvel; Quisnon; NM-441; Prulifloxacin [INN]; Sword; NM 441; NM-441
Cat No.:V6391 Purity: ≥98%
Prulifloxacin (NM441) is an orally bioactive fluoroquinolone antibiotic (antibiotic) with broad activity against Gram-positive (Gram+) and Gram-negative (Gram-) bacteria.
Prulifloxacin
Prulifloxacin Chemical Structure CAS No.: 123447-62-1
Product category: New12
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
Other Sizes
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text

 

  • Business Relationship with 5000+ Clients Globally
  • Major Universities, Research Institutions, Biotech & Pharma
  • Citations by Top Journals: Nature, Cell, Science, etc.
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description
Prulifloxacin (NM441) is an orally bioactive fluoroquinolone antibiotic (antibiotic) with broad activity against Gram-positive (Gram+) and Gram-negative (Gram-) bacteria. Prulifloxacin is the precursor of thiazolequinoline carboxylic acid analogue Ulifloxacin (NM394). Prulifloxacin may be utilized in lower urinary tract infections and chronic bronchitis.
Biological Activity I Assay Protocols (From Reference)
Targets
Fluoroquinolone antibiotic
ln Vitro
Minimum inhibitory concentrations (MICs) and mutant prevention concentrations (MPCs) of prulifloxacin against 30 strains of Escherichia coli isolated from urinary tract infections as well as the 'biological cost' related to acquisition of resistance to the same drug in 10 uropathogenic E. coli were assessed. In terms of MIC(90), prulifloxacin was more potent than ciprofloxacin and levofloxacin. Prulifloxacin produced lower or equal MPC values than the other two fluoroquinolones (93.3% and 73.3% compared with levofloxacin and ciprofloxacin, respectively). Compared with susceptible strains, prulifloxacin-resistant mutants showed a reduced rate of growth (ranging from 20.0% to 98.0% in different culture media and incubation conditions) and a decreased fitness index (ranging from 0.959 to 0.999). They were also impaired in their ability to adhere to uroepithelial cells and urinary catheters (11.7-66.4% and 16.3-78.3% reduction, respectively) and showed a lower surface hydrophobicity (51.2-76.0%). They were more susceptible to ultraviolet irradiation (30.6-93.8% excess mortality), showed increased resistance to colicins and diminished transfer of plasmids (<1-8.5x10(-8) vs. 3.3x10(-7)-2.4x10(-4)). Synthesis of haemolysin and type I fimbriae and production of flagella were also adversely affected. This study demonstrates a strict relationship between acquisition of prulifloxacin resistance and loss of important virulence traits. In this transition, E. coli pays a severe biological cost that entails a general reduction of fitness, thus compromising competition with susceptible wild-type strains in the absence of the drug[3].
ln Vivo
The peak plasma concentration of NM394 was 2.39 μg/ml following oral administration of NM441 at a dose of 20 mg/kg to dogs, as opposed to 0.63 μg/ml when NM394 was given alone. For treating Staphylococcus aureus-caused systemic infections, NM441 is twice as effective as ciprofloxacin and as effective as ofloxacin. In terms of efficacy against streptococcal infections, NM441 outperforms ofloxacin by two to three times and ciprofloxacin by five times [1].
Animal Protocol
NM441 is a lipophilic prodrug of a new thiazeto-quinoline carboxylic acid derivative NM394, and when it is administered orally it is readily absorbed and hydrolyzed to its parent compound. After oral administration of NM441 at a dose of 20 mg/kg to dogs, the peak concentration of NM394 in plasma was 2.39 micrograms/ml, whereas it was 0.63 micrograms/ml for NM394 administered alone. The in vivo activity of NM441 was compared with those of ciprofloxacin, ofloxacin, and enoxacin in mouse protection studies. NM441 was as effective as ofloxacin and was twice as effective as ciprofloxacin against systemic infection with Staphylococcus aureus. Against infections with streptococci, NM441 was two to three times as effective as ofloxacin and five times as effective as ciprofloxacin. Against infection with Escherichia coli, NM441 was as effective as ciprofloxacin and ofloxacin, but against infections with Klebsiella pneumoniae, Serratia marcescens, and Pseudomonas aeruginosa, NM441 was two to four times as effective as ciprofloxacin and ofloxacin. NM441 was three to seven times as effective as enoxacin in systemic infections. Against urinary tract infections with E. coli, NM441 reduced the number of bacterial CFU per gram of kidney by 1 to 2 log10 more and, with P. aeruginosa, by 1 to 6 log10 more than did ciprofloxacin and ofloxacin. Against respiratory tract infections with K. pneumoniae, NM441 was as effective as ofloxacin and was twice as effective as ciprofloxacin[1].
References
[1]. M Ozaki, et al. In vivo evaluation of NM441, a new thiazeto-quinoline derivative. Antimicrob Agents Chemother. 1991 Dec;35(12):2496-9.
[2]. Guillem Prats, et al. Prulifloxacin: a new antibacterial fluoroquinolone. Expert Rev Anti Infect Ther. 2006 Feb;4(1):27-41.
[3]. In vitro activity of prulifloxacin against Escherichia coli isolated from urinary tract infections and the biological cost of prulifloxacin resistance. Int J Antimicrob Agents . 2007 Jun;29(6):679-87.
[4]. Correlation among the toxicity profiling (28-days repeated oral dose toxicity), toxicokinetics and tissue distribution data of ulifloxacin, the active metabolite of prulifloxacin in Wistar albino rats. Environ Toxicol Pharmacol . 2012 Sep;34(2):588-607.
Additional Infomation
Prulifloxacin is a quinolone antibiotic and a fluoroquinolone antibiotic.
Prulifloxacin has been investigated for the treatment of Urinary Tract Infection.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Exact Mass
461.105
Elemental Analysis
C, 54.66; H, 4.37; F, 4.12; N, 9.11; O, 20.80; S, 6.95
CAS #
123447-62-1
PubChem CID
65947
Appearance
Typically exists as off-white to light yellow solids at room temperature
Density
1.6±0.1 g/cm3
Boiling Point
633.2±65.0 °C at 760 mmHg
Melting Point
211-214°C
Flash Point
336.8±34.3 °C
Vapour Pressure
0.0±2.0 mmHg at 25°C
Index of Refraction
1.721
LogP
3.27
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
11
Rotatable Bond Count
4
Heavy Atom Count
32
Complexity
931
Defined Atom Stereocenter Count
0
InChi Key
PWNMXPDKBYZCOO-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H20FN3O6S/c1-10-16(31-21(29)30-10)9-23-3-5-24(6-4-23)15-8-14-12(7-13(15)22)18(26)17(20(27)28)19-25(14)11(2)32-19/h7-8,11H,3-6,9H2,1-2H3,(H,27,28)
Chemical Name
6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl]-4-oxo-1H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
Synonyms
Prulifloxacin;NM441; Pruvel; Quisnon; NM-441; Prulifloxacin [INN]; Sword; NM 441; NM-441
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~12.5 mg/mL (~27.09 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.25 mg/mL (2.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01231737 UNKNOWN STATUS Drug: prulifloxacin Urinary Tract Infection University Of Perugia 2010-11 Phase 2
NCT03201796 COMPLETED Drug: Prulifloxacin 600 mg
Drug: Levofloxacin 500mg
Chronic Bacterial Prostatitis Aziende Chimiche Riunite Angelini Francesco S.p.A 2016-02-02 Phase 2
NCT02439632 COMPLETED Drug: prulifloxacin
Drug: Levofloxacin
Drug: Prulifloxacin Placebo
Drug: Levofloxacin Placebo
Acute Lower Urinary Tract Infection Lee's Pharmaceutical Limited 2014-02 Phase 3
NCT00448422 COMPLETED Drug: prulifloxacin Acute Bacterial Gastroenteritis Optimer Pharmaceuticals LLC, a subsidiary of Merck & Co., Inc 2006-12 Phase 3
NCT02157571 UNKNOWN STATUS Drug: Prulifloxacin
Drug: Levofloxacin
Drug: Levofloxacin Placebo
Drug: Prulifloxacin placebo
Acute Exacerbations of Chronic Bronchitis Lee's Pharmaceutical Limited 2013-06 Phase 3
Contact Us