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Purity: ≥98%
Delafloxacin (formerly also known as ABT-492, RX-3341; WQ-3034; trade name: Baxdela) is a novel quinolone-based antibiotic with potent activity against gram-positive, gram-negative, and atypical pathogens. Delafloxacin was approved in 2017 by FDA to treat patients with acute bacterial skin infections. ABT-492 demonstrated potent activity against penicillin-sensitive, penicillin-resistant, and levofloxacin-resistant Streptococcus pneumoniae strains (MICs ranging from 0.0078 to 0.125 micro g/ml); beta-lactamase-positive and beta-lactamase-negative Haemophilus influenzae strains (MICs ranging from 0.000313 to 0.00125 micro g/ml); and beta-lactamase-positive and beta-lactamase-negative Moraxella catarrhalis strains (MICs ranging from 0.001 to 0.0025 micro g/ml), with MICs being much lower than those of levofloxacin. Both ABT-492 and levofloxacin demonstrated concentration-dependent bactericidal activities in time-kill kinetics studies at four and eight times the MIC with 10 of 12 bacterial isolates exposed to ABT-492 and with 12 of 12 bacterial isolates exposed to levofloxacin.
| Targets |
Quinolone
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|---|---|
| ln Vivo |
in stable cell lines that express HCV replicons that encode renilla luciferase (Huh-7-Lunet or Huh7-1C cells). Across genotypes 1 through 6, vitilaprevir demonstrates strong pangenotypic antiviral activity, with an EC50 ranging from 0.33 to 6.6 nM. Voxilaprevir has IC50 values of 0.33 nM, 3.9 nM, 3.3 nM, 3.7 nM, 4.5 nM, 1.8 nM, and 6.6 nM, 1.9 nM against HCV replicon strains DQ314805, H77, Con1, JFH-1, J6, J8 (full length), and HM568433, SA13 (NS3 Chimera), respectively[1].
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| Animal Protocol |
Animal Model: Mice with a neutropenic murine lung infection model (four S. aureus , four S. pneumoniae, and four K. pneumoniae strains)[1]
Dosage: The total daily doses vary from 0.156 to 640 mg/kg/24 h Administration: 0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection Result: Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively. Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively. Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively. |
| References |
| Molecular Formula |
C18H12CLF3N4O4
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|---|---|
| Molecular Weight |
440.76
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| Exact Mass |
440.05
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| Elemental Analysis |
C, 49.05; H, 2.74; Cl, 8.04; F, 12.93; N, 12.71; O, 14.52
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| CAS # |
189279-58-1
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| Related CAS # |
Delafloxacin meglumine;352458-37-8;Delafloxacin-d5
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| Appearance |
White to off-white solid powder.
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| SMILES |
O=C(C1=CN(C2=NC(N)=C(F)C=C2F)C3=C(C=C(F)C(N4CC(O)C4)=C3Cl)C1=O)O
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| InChi Key |
DYDCPNMLZGFQTM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12ClF3N4O4/c19-12-13-7(1-9(20)14(12)25-3-6(27)4-25)15(28)8(18(29)30)5-26(13)17-11(22)2-10(21)16(23)24-17/h1-2,5-6,27H,3-4H2,(H2,23,24)(H,29,30)
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| Chemical Name |
1-(6-Amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
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| Synonyms |
Trade name. Baxdela; ABT-492; RX 3341; WQ-3034; ABT 492; RX3341; WQ3034; ABT492; RX-3341; WQ 3034
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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 |
| 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 : 88~100 mg/mL ( 199.65~226.88 mM )
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2688 mL | 11.3440 mL | 22.6881 mL | |
| 5 mM | 0.4538 mL | 2.2688 mL | 4.5376 mL | |
| 10 mM | 0.2269 mL | 1.1344 mL | 2.2688 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.
Time-kill curves for four clinical isolates. Curves on the left represent the activity of ABT-492, and the curves on the right represent the activity of levofloxacin against the same isolate.Antimicrob Agents Chemother.2004 Jan;48(1):203-8. |
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Composite concentration-response curves for penicillin-sensitiveS. pneumoniae(SPS) and penicillin-resistantS. pneumoniae(SPR) isolates following antibiotic exposure to ABT-492 (left-hand side) and levofloxacin (right-hand side) at 4, 6, and 12 h.Antimicrob Agents Chemother.2004 Jan;48(1):203-8. |
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