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| Targets |
Bacterial DNA gyrase and topoisomerase IV. Pazufloxacin Mesylate is a fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that introduces negative supercoils into DNA, which is critical for DNA replication and transcription. Topoisomerase IV is involved in the decatenation of replicated DNA chromosomes. By inhibiting these enzymes, Pazufloxacin Mesylate blocks DNA replication and transcription, leading to bacterial cell death. The compound inhibits DNA gyrase with IC50 values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin Mesylate is indicated for the treatment of respiratory tract infections, endometritis, prostatitis, cystitis, pyelonephritis, and liver abscess.
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| ln Vitro |
Pazufloxacin Mesylate demonstrates antibacterial activity in vitro against a range of gram-negative and gram-positive bacteria. The compound inhibits DNA gyrase with IC50 values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). Pazufloxacin Mesylate's antibacterial activity is assessed by standard antimicrobial susceptibility testing methods (broth microdilution or agar diffusion). The compound is active against pathogens causing respiratory tract infections, urinary tract infections, and other infections. Pazufloxacin Mesylate is a fluoroquinolone antibiotic.
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| ln Vivo |
Pazufloxacin Mesylate is used clinically for the treatment of respiratory tract infections including lung abscess and pneumonia, endometritis, prostatitis, cystitis, pyelonephritis, and liver abscess. The compound is administered orally. Its in vivo efficacy has been established through clinical use. Pazufloxacin Mesylate is a fluoroquinolone antibiotic.
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| Enzyme Assay |
Antibacterial susceptibility testing is performed using broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial strains (e.g., E. coli ATCC 25922, P. aeruginosa ATCC 27853) are cultured in appropriate media. Pazufloxacin Mesylate is serially diluted and tested against the bacteria. MIC values are determined as the lowest concentration causing complete inhibition of visible growth. DNA gyrase inhibition assays are performed using purified DNA gyrase and supercoiled DNA substrates. Quality control strains are included to ensure assay validity.
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| Cell Assay |
Antibacterial activity is evaluated in bacterial cell cultures using standard microbiological methods. Broth microdilution assays are performed in 96-well plates with appropriate media. Bacteria are cultured to logarithmic phase and diluted to a standard inoculum. Pazufloxacin Mesylate is serially diluted and added to wells. Plates are incubated at 35°C for 16-20 hours. MIC values are determined visually or using a microplate reader. Each experiment includes quality control strains and antibiotic standards.
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| Animal Protocol |
In vivo efficacy of Pazufloxacin Mesylate is evaluated in animal models of bacterial infection. The compound is administered orally at doses determined by preclinical studies. Bacterial burden is quantified in infected tissues by CFU plating. Clinical symptoms are monitored. Sample sizes typically range from 6-10 animals per group. Clinical studies have been conducted for respiratory tract infections, urinary tract infections, and other infections.
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| ADME/Pharmacokinetics |
Molecular Weight: 414.40. Formula: C16H15FN2O4·CH4O3S. CAS No.: 163680-77-1. IUPAC Name: (S)-(-)-10-(1-Aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3,de][1,4]benzoxazine-6-carboxylic acid methanesulfonate. Synonyms: Pazufloxacin Mesylate; Pazufloxacin methanesulfonate. Appearance: White to orange to green powder to crystal. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Typically at room temperature. Pazufloxacin Mesylate is an orally active fluoroquinolone antimicrobial agent.
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| Toxicity/Toxicokinetics |
Pazufloxacin Mesylate is generally well-tolerated at therapeutic doses. Common adverse effects may include gastrointestinal disturbances, headache, dizziness, and photosensitivity. As a fluoroquinolone, it may cause tendinitis and tendon rupture. It is contraindicated in patients with quinolone hypersensitivity. Standard toxicology studies have demonstrated an acceptable safety profile for its approved uses. Pazufloxacin Mesylate is approved for clinical use in many countries.
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| References |
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| Additional Infomation |
Pazufloxacin Mesylate is also known as Pazufloxacin methanesulfonate. Its IUPAC name is (S)-(-)-10-(1-Aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3,de][1,4]benzoxazine-6-carboxylic acid methanesulfonate. Pazufloxacin Mesylate is an orally active fluoroquinolone antimicrobial agent. It inhibits DNA gyrase with IC50 values of 0.88 μg/mL (E. coli) and 1.9 μg/mL (P. aeruginosa). It is indicated for the treatment of respiratory tract infections, endometritis, prostatitis, cystitis, pyelonephritis, and liver abscess. Regulatory approvals exist in many countries. Pazufloxacin Mesylate is for research use only.
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| Molecular Formula |
C17H19FN2O7S
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|---|---|
| Molecular Weight |
414.4044
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| Exact Mass |
414.089
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| Elemental Analysis |
C, 49.27; H, 4.62; F, 4.58; N, 6.76; O, 27.03; S, 7.74
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| CAS # |
163680-77-1
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| Related CAS # |
Pazufloxacin;127045-41-4
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| PubChem CID |
6918232
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| Appearance |
Solid powder
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| Boiling Point |
531.5ºC at 760 mmHg
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| Melting Point |
>255°C (dec.)
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| Flash Point |
275.2ºC
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| Vapour Pressure |
4E-12mmHg at 25°C
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| LogP |
3.025
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
695
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C(C(C1=O)=CN2[C@@H](C)COC3=C(C4(N)CC4)C(F)=CC1=C23)O.CS(=O)(O)=O
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| InChi Key |
UDHGFPATQWQARM-FJXQXJEOSA-N
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| InChi Code |
InChI=1S/C16H15FN2O4.CH4O3S/c1-7-6-23-14-11(16(18)2-3-16)10(17)4-8-12(14)19(7)5-9(13(8)20)15(21)221-5(2,3)4/h4-5,7H,2-3,6,18H2,1H3,(H,21,22)1H3,(H,2,3,4)/t7-/m0./s1
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| Chemical Name |
(S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid compound with methanesulfonic acid (1
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| Synonyms |
Pazufloxacin Mesylate; Pazucross; Pasil; T-3762; T 3762; T3762
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~241.31 mM )
H2O : ≥ 100 mg/mL (~241.31 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 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 25.0 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: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (6.03 mM) Solubility in Formulation 5: 150 mg/mL (361.96 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4131 mL | 12.0656 mL | 24.1313 mL | |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8263 mL | |
| 10 mM | 0.2413 mL | 1.2066 mL | 2.4131 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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