Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Targets |
Quinolone
|
---|---|
ln Vitro |
HepG2 cells exposed to trovafloxacin (20 µM; 24 hours) and tumor necrosis factor (TNF; 4 ng/mL) exhibit increased lactate dehydrogenase (LDH) leakage and apoptosis.After incubating HepG2 cells with trovafloxacin (20 µM) for 24 hours and TNF (4 ng/mL), the expression of early NF-κB-related factors A20 and IκBα is increased.In HepG2, trovafloxacin prolongs TNF-induced MAPK activation and IKKα/β activation[1].
Effectively preventing apoptotic cells from absorbing TO-PRO-3 is trovafloxacin. Moreover, trovafloxacin prevents apoptotic cells from releasing ATP. Trovafloxacin does not prevent PANX1 cleavage during apoptosis or caspase 3/7 activation[2]. With MICs of 0.06-0.25 mg/mL recorded for over 700 isolates, trovafloxacin is equally effective against pneumococci that are susceptible to penicillin as well as those that are resistant to it. Trovafloxacin's minimum inhibitory concentration (MIC) for 90% of pneumococci isolates is 0.125 μg/mL [3]. |
ln Vivo |
Treatment with trovafloxacin (150 mg/kg; oral; male C57BL/6 J mice) prevents the nuclear translocation of p65 that is induced by TNF. Treatment with trovafloxacin increases the expression of IκBα and A20, early NF-κB-related factors[1].When trovafloxacin is given to mice along with lipopolysaccharide (LPS) or tumor necrosis factor (TNF), it causes severe liver toxicity that is accompanied by large areas of the liver that are apoptotic, elevated serum levels of alanine amino transferases (ALT), and pro-inflammatory cytokines[1].
|
Animal Protocol |
Animal Model: Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion[1]
Dosage: 150 mg/kg Administration: Oral administration Result: revealed a higher proportion of cells in the liver with an elevated nuclear/cytoplasmic p65 ratio. |
References |
|
Molecular Formula |
C20H15F3N4O3
|
---|---|
Molecular Weight |
416.35
|
CAS # |
147059-72-1
|
Related CAS # |
Trovafloxacin mesylate;147059-75-4
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C1[C@@H]2[C@@H](C2N)CN1C3=C(C=C4C(=O)C(=CN(C4=N3)C5=C(C=C(C=C5)F)F)C(=O)O)F
|
InChi Key |
WVPSKSLAZQPAKQ-SOSAQKQKSA-N
|
InChi Code |
InChI=1S/C20H15F3N4O3/c21-8-1-2-15(13(22)3-8)27-7-12(20(29)30)17(28)9-4-14(23)19(25-18(9)27)26-5-10-11(6-26)16(10)24/h1-4,7,10-11,16H,5-6,24H2,(H,29,30)/t10-,11+,16
|
Chemical Name |
7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO : ~9.09 mg/mL (~21.83 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 | 2.4018 mL | 12.0091 mL | 24.0183 mL | |
5 mM | 0.4804 mL | 2.4018 mL | 4.8037 mL | |
10 mM | 0.2402 mL | 1.2009 mL | 2.4018 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.