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Clinafloxacin CI96 AM1091

CAS# 105956-97-6

Clinafloxacin CI96 AM1091

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Chemical Properties of Clinafloxacin CI96 AM1091

Cas No. 105956-97-6 SDF Download SDF
PubChem ID 60063 Appearance Powder
Formula C17H17ClFN3O3 M.Wt 365.8
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PD 127391
Solubility DMSO : 2 mg/mL (5.47 mM; ultrasonic and warming and heat to 80°C)
Chemical Name 7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid
SMILES C1CC1N2C=C(C(=O)C3=CC(=C(C(=C32)Cl)N4CCC(C4)N)F)C(=O)O
Standard InChIKey QGPKADBNRMWEQR-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H17ClFN3O3/c18-13-14-10(5-12(19)15(13)21-4-3-8(20)6-21)16(23)11(17(24)25)7-22(14)9-1-2-9/h5,7-9H,1-4,6,20H2,(H,24,25)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Clinafloxacin CI96 AM1091

DescriptionClinafloxacin(PD-127391) is a fluoroquinolone antibiotic. Target: Antibacterial Clinafloxacin is a broad-spectrum antibiotic of the quinolone carboxylic acid category currently in development for intravenous and oral therapy of serious infections [1]. Clinafloxacin is a novel fluoroquinolone with potent broad-spectrum in vitro activity against gram-positive, gram-negative, and anaerobic pathogens. Clinafloxacin is highly active against S. pneumoniae 7785 (MIC, 0.125 μg/mL), and neither gyrA nor parC quinolone resistance mutations alone have much effect on this activity [2]. Clinafloxacin is identified as the most active fluoroquinolone against S. pneumoniae when compared with ofloxacin, levofloxacin, sparfloxacin, grepafloxacin, and trovafloxacin and is currently being evaluated as an antipneumococcal agent [3].

References:
[1]. Humphrey, G.H., et al., Pharmacokinetics of clinafloxacin enantiomers in humans. J Clin Pharmacol, 1999. 39(11): p. 1143-50. [2]. Pan, X.S. and L.M. Fisher, DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother, 1998. 42(11): p. 2810-6. [3]. Jorgensen, J.H., et al., Activities of clinafloxacin, gatifloxacin, gemifloxacin, and trovafloxacin against recent clinical isolates of levofloxacin-resistant Streptococcus pneumoniae. Antimicrob Agents Chemother, 2000. 44(11): p. 2962-8.

Clinafloxacin CI96 AM1091 Dilution Calculator

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Preparing Stock Solutions of Clinafloxacin CI96 AM1091

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7337 mL 13.6687 mL 27.3373 mL 54.6747 mL 68.3434 mL
5 mM 0.5467 mL 2.7337 mL 5.4675 mL 10.9349 mL 13.6687 mL
10 mM 0.2734 mL 1.3669 mL 2.7337 mL 5.4675 mL 6.8343 mL
50 mM 0.0547 mL 0.2734 mL 0.5467 mL 1.0935 mL 1.3669 mL
100 mM 0.0273 mL 0.1367 mL 0.2734 mL 0.5467 mL 0.6834 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Clinafloxacin CI96 AM1091

Clinafloxacin is a fluoroquinolone that inhibits both Topo II (DNA gyrase)and topoisomerase IV dually in Streptococcus pneumoniae.

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References on Clinafloxacin CI96 AM1091

Clinafloxacin for Treatment of Burkholderia cenocepacia Infection in a Cystic Fibrosis Patient.[Pubmed:26722110]

Antimicrob Agents Chemother. 2015 Dec 31;60(1):1-5.

Respiratory infection with Burkholderia cenocepacia is associated with accelerated decline in lung function and increased mortality in cystic fibrosis (CF) patients (A. M. Jones, M. E. Dodd, J. R. W. Govan, V. Barcus, C. J. Doherty, J. Morris, and A. K. Webb, Thorax 59:948-951, 2004, http://dx.doi.org/10.1136/thx.2003.017210). B. cenocepacia often possesses innate resistance to multiple antimicrobial classes, making eradication uncommon in established infection (P. B. Davis, Am J Respir Crit Care Med 173:475-482, 2006, http://dx.doi.org/10.1164/rccm.200505-840OE). We report the use of clinafloxacin in a CF patient with advanced B. cenocepacia infection, present pharmacokinetic (PK) data, and discuss the potential therapeutic role of clinafloxacin in patients with this condition.

Heterologous strategy enhancing the sensitivity of the fluorescence polarization immunoassay of clinafloxacin in goat milk.[Pubmed:25914021]

J Sci Food Agric. 2016 Mar 15;96(4):1341-6.

BACKGROUND: Clinafloxacin is used for the treatment of disease in food-producing animals, e.g. Brucella melitensis, which often occurs in goats; however, the clinafloxacin residue in goat milk may harm human health and result in the development of drug-resistant bacterial strains or allergies. Despite this, there is not a rapid, sensitive and accurate analytical method in goat milk for rapid screening or monitoring purposes. RESULTS: One homologous and five heterologous tracers were designed and compared for fluorescence polarization immunoassay (FPIA) optimization. Based on the combination of a heterologous tracer (PAZ-FITC, synthesized with pazufloxacin and FITC) and the antibody against clinafloxacin, a highly sensitive FPIA was established for the detection of clinafloxacin residue in goat milk for the first time. The IC50 value was 29.3 microg L(-1) for clinafloxacin in the heterologous format - six times lower than that of the combination of the homologous tracers and the antibody. The recoveries ranged from 86.8% to 104.5%, with the relative standard deviation ranging from 4.1% to 7.2%. Validation by high-performance liquid chromatography (HPLC) confirmed that the results obtained from the proposed FPIA were in agreement with those of HPLC. CONCLUSION: This proposed heterologous strategy for enhanced FPIA is sensitive and rapid enough for the high-throughput detection of clinafloxacin residue in goat milk.

In vitro activity and rodent efficacy of clinafloxacin for bovine and swine respiratory disease.[Pubmed:23785362]

Front Microbiol. 2013 Jun 14;4:154.

Clinafloxacin is a broad-spectrum fluoroquinolone that was originally developed and subsequently abandoned in the late 1990s as a human health antibiotic for respiratory diseases. The purpose of this study was to investigate the activity of clinafloxacin as a possible treatment for respiratory disease in cattle and pigs. Minimum inhibitory concentration (MIC) values were determined using Clinical and Laboratory Standards Institute recommended procedures with recent strains from the Zoetis culture collection. Rodent efficacy was determined in CD-1 mice infected systemically or intranasally with bovine Mannheimia haemolytica or Pasteurella multocida, or swine Actinobacillus pleuropneumoniae, and administered clinafloxacin for determination of ED50 (efficacious dose-50%) values. The MIC90 values for clinafloxacin against bovine P. multocida, M. haemolytica, Histophilus somni, and M. bovis were 0.125, 0.5, 0.125, and 1 mug/ml, respectively, and the MIC90 values against swine P. multocida, A. pleuropneumoniae, S. suis, and M. hyopneumoniae were i0.03, i0.03, 0.125, and i0.008 mug/ml, respectively. Efficacy in mouse models showed average ED50 values of 0.019 mg/kg/dose in the bovine M. haemolytica systemic infection model, 0.55 mg/kg in the bovine P. multocida intranasal lung challenge model, 0.08 mg/kg/dose in the bovine P. multocida systemic infection model, and 0.7 mg/kg/dose in the swine A. pleuropneumoniae systemic infection model. Clinafloxacin shows good in vitro activity and efficacy in mouse models and may be a novel treatment alternative for the treatment of respiratory disease in cattle and pigs.

Synthesis of (99m)TcN-clinafloxacin Dithiocarbamate Complex and Comparative Radiobiological Evaluation in Staphylococcus aureus Infected Mice.[Pubmed:25538485]

World J Nucl Med. 2014 Sep;13(3):154-8.

Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through [(99m)Tc identical with N](2+) core with the gamma (gamma) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) identical with N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 +/- 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) identical with N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 +/- 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.s., h.s., higher S.a. (live) up take with specific and targeted in vivo distribution confirmed potentiality of the (99m)Tc(V) identical with N-CNND complex as perspective S.a. in vivo infection radiotracer.

Description

Clinafloxacin(PD-127391) is a fluoroquinolone antibiotic.

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