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Lomefloxacin HCl

CAS# 98079-52-8

Lomefloxacin HCl

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Lomefloxacin HCl

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Chemical Properties of Lomefloxacin HCl

Cas No. 98079-52-8 SDF Download SDF
PubChem ID 68624 Appearance Powder
Formula C17H20ClF2N3O3 M.Wt 387.81
Type of Compound N/A Storage Desiccate at -20°C
Solubility H2O : 10 mg/mL (25.79 mM; Need ultrasonic and warming)
Chemical Name 1-ethyl-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;hydrochloride
SMILES [H+].[Cl-].CCN1C=C(C(O)=O)C(=O)c2cc(F)c(N3CCNC(C)C3)c(F)c12
Standard InChIKey KXEBLAPZMOQCKO-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H19F2N3O3.ClH/c1-3-21-8-11(17(24)25)16(23)10-6-12(18)15(13(19)14(10)21)22-5-4-20-9(2)7-22;/h6,8-9,20H,3-5,7H2,1-2H3,(H,24,25);1H
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 Lomefloxacin HCl

DescriptionLomefloxacin HCl is a fluoroquinolone antibiotic. Target: Antibacterial Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited [1].

References:
[1]. http://www.drugbank.ca/drugs/DB00978

Lomefloxacin HCl Dilution Calculator

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Lomefloxacin HCl Molarity Calculator

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Preparing Stock Solutions of Lomefloxacin HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5786 mL 12.8929 mL 25.7858 mL 51.5716 mL 64.4646 mL
5 mM 0.5157 mL 2.5786 mL 5.1572 mL 10.3143 mL 12.8929 mL
10 mM 0.2579 mL 1.2893 mL 2.5786 mL 5.1572 mL 6.4465 mL
50 mM 0.0516 mL 0.2579 mL 0.5157 mL 1.0314 mL 1.2893 mL
100 mM 0.0258 mL 0.1289 mL 0.2579 mL 0.5157 mL 0.6446 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 Lomefloxacin HCl

Lomefloxacin HCl is a fluoroquinolone antibiotic.

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References on Lomefloxacin HCl

Enhancement of lomefloxacin Hcl ocular efficacy via niosomal encapsulation: in vitro characterization and in vivo evaluation.[Pubmed:27241274]

J Liposome Res. 2017 Dec;27(4):312-323.

The aim of this study is to develop and evaluate niosomal dispersions loaded with the hydrophilic drug; Lomefloxacin HCl (LXN) for the management of ocular bacterial conjunctivitis. LXN-loaded niosomes were prepared by the thin film hydration method following a full factorial formulation design. Two independent variables were evaluated: the type of surfactant (X1) and the surfactant:cholesterol ratio (X2). The dependent variables comprised entrapment efficiency (EE%: Y1), particle size (PS: Y2) and zeta potential (ZP: Y3). The optimum formulation, N-LXN14 (Tw60: CH, 1:1), was spherical in shape and exhibited EE% of 68.41 +/- 0.07, PS of 176.0 +/- 0.98 and ZP of -40.70 +/- 2.20 with a sustained release profile over 8 hours following the Higuchi model. N-LXN14 proved good physicochemical stability under refrigeration up to 3 months. Ocular irritancy test showed no signs of ocular toxicity, confirming the safety and suitability for ocular application. Microbiological evaluation of the antibacterial effect of N-LXN14 was conducted using the susceptibility test and through the induction of topical conjunctivitis by Staphylococcus aureus (S. aureus) followed by topical therapy. Susceptibility test manifested significantly higher percent inhibition of S. aureus and higher AUC0-12 h of N-LXN14 (604.59 +/- 0.05) compared to the commercial product (126.25 +/- 0.049). Both clinical observation and colony count of the infected eyes after eight days of treatment demonstrated significant improvement in therapeutic response. The infected eyes were completely healed with eradication of S. aureus. In conclusion, the results showed that LXN niosomal dispersions may serve as a promising superior ocular delivery system in the treatment of bacterial conjunctivitis.

Design and evaluation of proniosomes as a carrier for ocular delivery of lomefloxacin HCl.[Pubmed:27079800]

J Liposome Res. 2017 Jun;27(2):118-129.

The current investigation aims to develop and evaluate novel ocular proniosomal gels of Lomefloxacin HCl (LXN); in order to improve its ocular bioavailability for the management of bacterial conjunctivitis. Proniosomes were prepared using different types of nonionic surfactants solely and as mixtures with Span 60. The formed gels were characterized for entrapment efficiency, vesicle size, and in vitro drug release. Only Span 60 was able to form stable LXN-proniosomal gel when used individually while the other surfactants formed gels only in combination with Span 60 at different ratios. The optimum proniosomal gel; P-LXN 7 (Span 60:Tween 60, 9:1) appeared as spherical shaped vesicles having high entrapment efficiency (>80%), appropriate vesicle size (187 nm) as well as controlled drug release over 12 h. Differential scanning calorimetry confirmed the amorphous nature of LXN within the vesicles. Stability study did not show any significant changes in entrapment efficiency or vesicle size after storage for 3 months at 4 degrees C. P-LXN 7 was found to be safe and suitable for ocular delivery as proven by the irritancy test. The antibacterial activity of P-LXN 7 evaluated using the susceptibility test and topical therapy of induced ocular conjunctivitis confirmed the enhanced antibacterial therapeutic efficacy of the LXN-proniosomal gel compared to the commercially available LXN eye drops.

Description

Lomefloxacin hydrochloride is a fluoroquinolone antibiotic.

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