The antibiotic sparfloxacin (CI-978) has strong and widespread antibacterial action. Ninety percent of the strains tested had minimum inhibitory concentrations (MICs) ranging from 0.1 to 0.78 μg/ml against Gram-positive bacteria, including Streptococcus, Enterococcus, and Staphylococcus spp., and MICs ranging from 0.1 to 0.78 μg/ml against Gram-negative bacteria, including Staphylococcus spp. The Pseudomonas genus and Enterobacteriaceae family contain 0.0125 to 1.56 μg/ml. Its minimum inhibitory concentration (MIC) ranges from 0.025 to 0.78 μg/ml for glucose-nonfermenting bacteria, 0.2 to 0.78 μg/ml for anaerobic bacteria, and 0.0125 to 0.05 μg/ml for Legionella. In mice, systemic infections caused by Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, and Pseudomonas aeruginosa have been effectively treated with sparfloxacin (CI-978) when administered orally [1]. DNA synthesis is inhibited by sparfloxacin, which targets DNA gyrase [2].

Absorption, Distribution and Excretion
Absorbed well after oral administration, with an absolute oral bioavailability of 92%. Co-administration with milk or food does not affect its absorption; however, concurrent use with antacids containing magnesium hydroxide and aluminum hydroxide can reduce the oral bioavailability of sparfloxacin by up to 50%. Metabolism/Metabolites Hepatic metabolism. Primarily metabolized to glucuronide conjugates via phase II glucuronidation. Metabolism does not utilize or interferes with the cytochrome P450 enzyme system. Biological Half-Life Mean terminal elimination half-life is 20 hours (range 16-30 hours). The half-life is prolonged in patients with renal impairment (creatinine clearance < 50 mL/min).

Use of Sparfloxacin during Pregnancy and Lactation ◉ Overview of Use During Lactation There is currently no information regarding the use of sparfloxacin during lactation. Traditionally, fluoroquinolones are not recommended for use in infants due to concerns about adverse effects on the developing joints of infants. However, recent studies suggest the risk is minimal. Calcium in breast milk may prevent the absorption of small amounts of fluoroquinolones in breast milk, but there is currently insufficient data to confirm or refute this claim. Lactating women can use sparfloxacin, but close monitoring of the infant's gut microbiota is necessary, for example, for changes in diarrhea or candidiasis (thrush, diaper rash). However, alternative medications with available safety information are preferred. ◉ Effects on Breastfed Infants No published information was found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information was found as of the revision date.

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Protein Binding Serum plasma protein binding is low, approximately 45%.

[1]. In vitro and in vivo antibacterial activities of AT-4140, a new broad-spectrum quinolone. Antimicrob Agents Chemother, 1989. 33(8): p. 1167-73.

[2]. Pan, X.S. and L.M. Fisher, Targeting of DNA gyrase in Streptococcus pneumoniae by sparfloxacin: selective targeting of gyrase or topoisomerase IV by quinolones. Antimicrob Agents Chemother, 1997. 41(2): p. 471-4.

Sparfloxacin is a quinolone antibiotic, belonging to the quinolone monocarboxylic acid class, N-arylpiperazine class, quinolone antibiotics, and fluoroquinolone antibiotics. Sparfloxacin is a fluoroquinolone antibiotic used to treat bacterial infections. It exerts its antibacterial activity by inhibiting bacterial topoisomerase DNA gyrase. DNA gyrase is an important enzyme that controls DNA topology and assists in DNA replication, repair, inactivation, and transcription. Sparfloxacin is a fluoroquinolone antibiotic that inhibits DNA replication and transcription by inhibiting bacterial DNA gyrase. Due to its high rate of phototoxicity, sparfloxacin has been withdrawn from the US market. Drug Indications This drug is indicated for the treatment of the following adult infections caused by susceptible strains of microorganisms: community-acquired pneumonia (caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae) and acute bacterial exacerbations of chronic bronchitis (caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae). FDA Label Mechanism of Action Sparfloxacin's bactericidal action derives from the inhibition of topoisomerase II (DNA gyrase) and topoisomerase IV, two enzymes essential for bacterial DNA replication, transcription, repair, and recombination. Pharmacodynamics Sparfloxacin is a synthetic broad-spectrum fluoroquinolone antibacterial drug, belonging to the same class as ofloxacin and norfloxacin. Sparfloxacin exhibits in vitro activity against a variety of Gram-negative and Gram-positive bacteria. Sparfloxacin exerts its antibacterial effect by inhibiting the bacterial topoisomerase DNA gyrase. DNA gyrase is an important enzyme that controls DNA topology and assists in DNA replication, repair, inactivation, and transcription. Quinolones have different chemical structures and mechanisms of action than β-lactam antibiotics. Therefore, quinolones may be effective against bacteria resistant to β-lactam antibiotics. Although cross-resistance between sparfloxacin and other fluoroquinolones has been observed, some microorganisms resistant to other fluoroquinolones may be sensitive to sparfloxacin. In vitro studies have shown that sparfloxacin, in combination with rifampin, has antagonistic effects against Staphylococcus aureus.

C19H22F2N4O3

392.3998

392.165

110871-86-8

60464

Light yellow to yellow solid powder

1.4±0.1 g/cm3

640.4±55.0 °C at 760 mmHg

265°C

341.1±31.5 °C

0.0±2.0 mmHg at 25°C

1.627

1.2

3

9

3

28

691

2

C[C@@H]1CN(C[C@@H](N1)C)C2=C(C(=C3C(=C2F)N(C=C(C3=O)C(=O)O)C4CC4)N)F

DZZWHBIBMUVIIW-DTORHVGOSA-N

InChI=1S/C19H22F2N4O3/c1-8-5-24(6-9(2)23-8)17-13(20)15(22)12-16(14(17)21)25(10-3-4-10)7-11(18(12)26)19(27)28/h7-10,23H,3-6,22H2,1-2H3,(H,27,28)/t8-,9+

5-amino-1-cyclopropyl-7-((3S,5R)-3,5-dimethylpiperazin-1-yl)-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

CI 978 CI-978 CI978 Sparfloxacin Esparfloxacino Zagam

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

0.1 M NaOH : ~50 mg/mL (~127.42 mM)
DMSO : ~3.33 mg/mL (~8.49 mM)
H2O : ~0.67 mg/mL (~1.71 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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