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| 25mg |
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Purity: ≥98%
Delafloxacin MEGLUMINE (WQ-3034; ABT-492; RX-3341; WQ3034; ABT492; RX3341; Baxdela), the MEGLUMINE salt of Delafloxacin, is an antibiotic of the quinolone class approved in 2017 by FDA to treat patients with acute bacterial skin infections. It is effective against gram-positive, gram-negative, and atypical pathogens.
| Targets |
Quinolone
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|---|---|
| ln Vitro |
Delafloxacin is very effective against S. aureus; total daily doses range from 0.156 to 640 mg/kg/24 h, subcutaneous injection. Even at the lowest dose tested, a reduction in the organism burden from untreated controls of 1.5 to 2.2 log10 CFU is seen against all four strains, and for two strains (MW2 and R2527), there is net bactericidal activity at the lowest dose. All S. aureus strains have a >4-log10 kill from initial burden at the maximum doses examined[1].
The moderate terminal elimination half-life of delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) is [1] (t1/2=0.68 h, 0.79 h, 0.69 h, and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively).
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| ln Vivo |
Delafloxacin is very effective against Staphylococcus aureus. The recommended daily dose is 0.156 to 640 mg/kg/24 hours administered subcutaneously. Even at the lowest dose investigated, for all four strains, there was a decrease in the organism burden of 1.5 to 2.2 log10 CFU relative to the untreated control; additionally, for two strains (MW2 and R2527), at the lowest Net bactericidal activity occurs at the dose. Initial loading of all S. aureus strains had >4-log10 death rates at the highest dose under investigation [1]. Delafloxacin has an intermediate terminal elimination half-life (t1/2 for 2.5 mg/kg = 0.68 hours, 0.79 hours, 0.69 hours, and 1.0 hours, 10 mg/kg, 40 mg/kg, and 160 mg/kg; SC, 24 hours) [1].
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| Animal Protocol |
Animal/Disease Models: neutropenic mice [1]
Doses: 2.5, 10, 40, 160 mg/kg; 0.2 mL Route of Administration: subcutaneous injection; 24-hour Experimental Results: Maximum drug concentration (Cmax) concentration range is 2 to 71 mg/L. AUC0-∞ values ranged from 2.8 to 152 mg·h/L and were linear over the dose range of 2.5 to 160 mg. Elimination half-life (t1/2) ranges from 0.7 to 1 hour. |
| References |
[1]. Lepak AJ, et al. In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4764-9.
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| Molecular Formula |
C25H29CLF3N5O9
|
|---|---|
| Molecular Weight |
635.986
|
| Elemental Analysis |
C, 47.21; H, 4.60; Cl, 5.57; F, 8.96; N, 11.01; O, 22.64
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| CAS # |
352458-37-8
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| Related CAS # |
Delafloxacin;189279-58-1
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| Appearance |
Solid powder
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| SMILES |
CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.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 |
AHJGUEMIZPMAMR-WZTVWXICSA-N
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| InChi Code |
InChI=1S/C18H12ClF3N4O4.C7H17NO5/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;1-8-2-4(10)6(12)7(13)5(11)3-9/h1-2,5-6,27H,3-4H2,(H2,23,24)(H,29,30);4-13H,2-3H2,1H3/t;4-,5+,6+,7+/m.0/s1
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| Chemical Name |
(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
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| Synonyms |
Trade name. Baxdela; ABT-492; ABT 492 meglumine; ABT492; RX-3341; WQ-3034; RX3341; WQ3034; RX 3341; WQ 3034 meglumine
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : 6.4~100 mg/mL ( 10.06~157.24 mM )
Water : 50~100 mg/mL(78.62 mM) |
|---|---|
| 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 | 1.5724 mL | 7.8618 mL | 15.7235 mL | |
| 5 mM | 0.3145 mL | 1.5724 mL | 3.1447 mL | |
| 10 mM | 0.1572 mL | 0.7862 mL | 1.5724 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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