2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Topoisomerase Antibiotic
  4. Trovafloxacin mesylate

Trovafloxacin (mesylate)  (Synonyms: メシル酸トロバフロキサシン)

製品番号: HY-103399 純度: 99.76%
COA 取扱説明書 Technical Support

Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.

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Trovafloxacin mesylate

Trovafloxacin (mesylate) 構造式

CAS 番号 : 147059-75-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 101 在庫あり
Solution
10 mM * 1 mL in DMSO USD 101 在庫あり
Solid
5 mg $90 在庫あり
10 mg $150 在庫あり
25 mg $322 在庫あり
50 mg $550 在庫あり
100 mg $880 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 7 publication(s) in Google Scholar

Other Forms of Trovafloxacin mesylate:

Trovafloxacin (mesylate) 関連抗体

Top Publications Citing Use of Products

Topoisomerase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Topoisomerase Topo I Topo II DNA gyrase

Antibiotic アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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製品説明

Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].

IC50 & Target

Quinolone

 

体外実験

Trovafloxacin (20 μM; 24 hours; HepG2 cells) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH) in HepG2 cells[1].
Trovafloxacin (20 μM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα[1].
Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2[1].
Trovafloxacin is a potent inhibitor of TO-PRO-3 uptake by apoptotic cells. Trovafloxacin also inhibits ATP release from apoptotic cells. Trovafloxacin does not inhibit caspase 3/7 activation, or caspase-mediated PANX1 cleavage during apoptosis[2].
Trovafloxacin is equally active against both penicillin-susceptible and -resistant pneumococci, with MICs of 0.06-0.25 mg/mL reported for more than 700 isolates. The MICs of Trovafloxacin at which 90% of isolates are inhibited for 55 isolates of pneumococci is 0.125 μg/mL[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trovafloxacin (mesylate) 関連抗体

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 20 µM
Incubation Time: 24 hours
Result: Showed a gradual increase of Annexin V-staining and an increased leakage of lactate dehydrogenase (LDH) at 24 h.

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: 20 µM
Incubation Time: 24 hours
Result: Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.
体内実験

Trovafloxacin (150 mg/kg; oral administration; male C57BL/6 J mice) treatment disrupts TNF-induced p65 nuclear translocation. Trovafloxacin treatment increases expression of early NF-κB-related factors A20 and IκBα[1].
Trovafloxacin, when administered in combination with lipopolysaccharide (LPS) or TNF to mice induces severe liver toxicity associated with vast apoptotic areas in the liver, increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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; once
Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
分子量

512.46

分子式

C21H19F3N4O6S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2=CC=C(F)C=C2F)C3=NC(N4C[C@@]5([H])[C@H](N)[C@@]5([H])C4)=C(F)C=C3C1=O)O.CS(=O)(O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
体外: 

DMSO : 116.67 mg/mL (227.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (39.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9514 mL 9.7569 mL 19.5137 mL
5 mM 0.3903 mL 1.9514 mL 3.9027 mL
10 mM 0.1951 mL 0.9757 mL 1.9514 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.76%

COA (254 KB) HNMR (145 KB) RP-HPLC (162 KB) NP-HPLC (127 KB) LCMS (106 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9514 mL 9.7569 mL 19.5137 mL 48.7843 mL
5 mM 0.3903 mL 1.9514 mL 3.9027 mL 9.7569 mL
10 mM 0.1951 mL 0.9757 mL 1.9514 mL 4.8784 mL
15 mM 0.1301 mL 0.6505 mL 1.3009 mL 3.2523 mL
20 mM 0.0976 mL 0.4878 mL 0.9757 mL 2.4392 mL
25 mM 0.0781 mL 0.3903 mL 0.7805 mL 1.9514 mL
30 mM 0.0650 mL 0.3252 mL 0.6505 mL 1.6261 mL
DMSO 40 mM 0.0488 mL 0.2439 mL 0.4878 mL 1.2196 mL
50 mM 0.0390 mL 0.1951 mL 0.3903 mL 0.9757 mL
60 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8131 mL
80 mM 0.0244 mL 0.1220 mL 0.2439 mL 0.6098 mL
100 mM 0.0195 mL 0.0976 mL 0.1951 mL 0.4878 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Trovafloxacin mesylate Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trovafloxacin147059-75-4BacterialTopoisomeraseAntibioticPANX1antibioticbroad-spectrumhepatotoxicityNF-κBLPSpro-inflammatoryTNFDNAgyrasetopoisomerase-IVpneumococciInhibitorinhibitorinhibit

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