NadifloxacinCAS# 124858-35-1 |
- SU14813
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| Cas No. | 124858-35-1 | SDF | Download SDF |
| PubChem ID | 4410 | Appearance | Powder |
| Formula | C19H21FN2O4 | M.Wt | 360.38 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | OPC7251 | ||
| Solubility | DMSO : 25 mg/mL (69.37 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| SMILES | CC1CCC2=C3N1C=C(C(=O)C3=CC(=C2N4CCC(CC4)O)F)C(=O)O | ||
| Standard InChIKey | JYJTVFIEFKZWCJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H21FN2O4/c1-10-2-3-12-16-13(18(24)14(19(25)26)9-22(10)16)8-15(20)17(12)21-6-4-11(23)5-7-21/h8-11,23H,2-7H2,1H3,(H,25,26) | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Nadifloxacin(OPC7251) is a topical fluoroquinolone antibiotic for the treatment of acne vulgaris.
Target: Antibacterial
Nadifloxacin is a potent, broad-spectrum, quinolone agent approved for topical use in acne vulgaris and skin infections. Nadifloxacin inhibits the enzyme DNA gyrase that is involved in bacterial DNA synthesis and replication, thus inhibiting the bacterial multiplication. In vitro studies of nadifloxacin show potent and broad-spectrum antibacterial activity against aerobic Gram-positive, Gram-negative and anaerobic bacteria. Additionally, studies also suggest that the effectiveness of nadifloxacin in inflammatory acne lesions may be attributed to its inhibitory effect on pro-inflammatory cytokines like interleukin (IL)-1α, IL-6, and IL-8 which also play an important role in acne pathogenesis [1, 2]. References: | |||||
Nadifloxacin Dilution Calculator
Nadifloxacin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7748 mL | 13.8742 mL | 27.7485 mL | 55.497 mL | 69.3712 mL |
| 5 mM | 0.555 mL | 2.7748 mL | 5.5497 mL | 11.0994 mL | 13.8742 mL |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL | 5.5497 mL | 6.9371 mL |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.555 mL | 1.1099 mL | 1.3874 mL |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.555 mL | 0.6937 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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Nadifloxacin is a topical fluoroquinolone antibiotic for the treatment of acne vulgaris.
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Clinical and bacteriological evaluation of adapalene 0.1% gel plus nadifloxacin 1% cream versus adapalene 0.1% gel in patients with acne vulgaris.[Pubmed:23724808]
J Dermatol. 2013 Aug;40(8):620-5.
This multicenter, randomized parallel group study investigated the efficacy and tolerability of adapalene 0.1% gel plus Nadifloxacin 1% cream (combination therapy) compared with adapalene gel (monotherapy) during 12-week treatment of acne vulgaris. A total of 184 Japanese patients aged above 12 years with moderate to severe acne as indicated by the Japanese severity grading criteria were randomized to combination therapy (n = 84) and monotherapy (n = 100) groups, both having comparable demographic and baseline characteristics. Adapalene was applied only to inflammatory acne lesions in order to minimize skin irritation and ensure the treatment results. Efficacy and safety evaluations, treatment compliance and satisfaction with drug application were periodically monitored. The combination therapy provided a significantly greater efficacy than adapalene in decrement of inflammatory papulopustular lesions at 4 weeks and thereafter (P = 0.0056). The overall judgment of the therapeutic efficacy by the physician at the end of study revealed a significant difference (P = 0.02496) between the groups in favor of combination therapy. Dryness was reported in a greater proportion of patients undergoing monotherapy than combination therapy at weeks 2 and 4 (P = 0.04652). The patient self-assessment in satisfaction with the drug application at the end of study revealed a significant difference (P = 0.00268) between the groups in favor of combination therapy. Among 76 strains of Propionibacterium acnes isolated from 87 patients, no strain was resistant to Nadifloxacin. Thus, the simultaneous use of adapalene and Nadifloxacin may provide an additive and complementary effect, resulting in clinical superiority and greater patient adherence compared to adapalene monotherapy.
Green Nail Syndrome (Pseudomonas aeruginosa Nail Infection): Two Cases Successfully Treated with Topical Nadifloxacin, an Acne Medication.[Pubmed:25202260]
Case Rep Dermatol. 2014 Jul 19;6(2):180-4.
Green nail syndrome (GNS) caused by Pseudomonas aeruginosa is the most common bacterial nail infection. The treatment of GNS is challenging in many cases and recommendations based on clinical trials are lacking. We report two cases with GNS successfully treated with off-label use of topical Nadifloxacin, a fluoroquinolone approved for acne and bacterial skin infections in some countries.
Efficacy and tolerability of topical fixed combination of nadifloxacin 1% and adapalene 0.1% in the treatment of mild to moderate acne vulgaris in Indian patients: a multicenter, open-labelled, prospective study.[Pubmed:25071260]
Indian J Dermatol. 2014 Jul;59(4):385-9.
BACKGROUND: A combination of topical retinoid and antibacterial therapy is often advocated for acne to enhance therapeutic efficacy. AIMS: A preliminary study to evaluate the efficacy and tolerability of a topical fixed combination of Nadifloxacin (1%) and adapalene (0.1%) in the treatment of mild to moderate acne in Indian patients. MATERIALS AND METHODS: This was an open-labeled, phase 3 non-randomized, non-comparative study conducted at five centers (Ahmedabad, Nagpur, Thane, Bangalore, and Mumbai) across India. Of 119 enrolled patients with mild to moderate acne, 117 patients were evaluated at the end of the study for efficacy parameters. A fixed combination of Nadifloxacin (1%) and adapalene (0.1%) topical gel was applied at the affected area once at night for a period of 8 weeks. Reduction in the total, inflammatory and non-inflammatory lesion counts from the baseline, investigator global assessment (IGA) and reduction in the severity of acne as per combined acne severity classification were the primary efficacy variables measured at 2 weeks, 4 weeks, and 8 weeks. RESULTS: Overall, 98.3% patients showed a statistically significant progressive reduction in non-inflammatory lesion counts, inflammatory lesion counts, and total lesion counts over the study duration. By the end of 8 weeks, 75% of the patients had their global assessment scores approaching to normal healthy skin score. The adverse events were mild to moderate in severity. CONCLUSION: This preliminary study shows that a fixed combination of 1% Nadifloxacin and 0.1% adapalene topical gel could be an effective and well-tolerated option for the treatment of mild to moderate acne vulgaris. However, further well-controlled, randomized and comparative evaluation of this combination is necessary.
Efficacy and safety of nadifloxacin for bacterial skin infections: results from clinical and post-marketing studies.[Pubmed:25212256]
Dermatol Ther (Heidelb). 2014 Dec;4(2):233-48.
INTRODUCTION: Skin and soft tissue infections involve microbial invasion of the skin and underlying soft tissues and are estimated to affect 7-10% of hospitalized patients worldwide. Nadifloxacin, a topical fluoroquinolone, has been shown to be effective against aerobic Gram-negative, Gram-positive (including MRSA and coagulase-negative staphylococci), and anaerobic bacteria. However, there is paucity of data comparing efficacy and safety of 1% Nadifloxacin with other anti-bacterials for skin infections in Indian patients. METHODS: This article presents the results of one post-marketing surveillance (PMS) and three randomized, open, non-blinded, multi-centric clinical studies that compared Nadifloxacin with mupirocin and framycetin, and Nadifloxacin with fusidic acid. Patients in India, aged from 1 to 65 years old, suffering from mild to moderate bacterial skin infections including impetigo, secondarily infected wounds, folliculitis, infected atopic dermatitis, and furunculosis were randomly allocated to three treatment groups within the studies. Efficacy was assessed by the evaluation of symptoms of erythema, exudation, swelling, pruritus, crusting, pain and tenderness in all the studies. RESULTS: A total of 272 subjects were enrolled in the study and subjects were randomly assigned to one of the three treatment groups; 92 in the Nadifloxacin group, 90 in the mupirocin group, and 90 in the framycetin group. A significant reduction in the mean scores for bacterial infection symptoms in the Nadifloxacin groups was observed when compared to mupirocin, framycetin and fusidic acid groups. Both physician and patients rated Nadifloxacin as excellent (complete remission of symptoms) on a 4-point scale in the studies. No adverse events (AEs) were reported in the clinical studies. In the PMS, only two patients (of 329, 0.6%) reported AEs including burning and itching, one in each patient that had resolved at the time of reporting. CONCLUSION: Nadifloxacin, a fluoroquinolone, is a new alternative topical agent in the treatment of bacterial skin infection with minimal AEs.
