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Roxithromycin (RU-28965) is an orally active semi-synthethic macrolideantibiotic. Roxithromycin inhibits protein biosynthesis in the elongation step by binding to 50S bacterial ribosome. Roxithromycin has antimicrobial, antiproliferative, anti-inflammatory, tumour vasculature inhibiting and lung injury ameliorating effects.
For research use only. We do not sell to patients.
Roxithromycin (RU-28965) is an orally active semi-synthethic macrolideantibiotic. Roxithromycin inhibits protein biosynthesis in the elongation step by binding to 50S bacterial ribosome. Roxithromycin has antimicrobial, antiproliferative, anti-inflammatory, tumour vasculature inhibiting and lung injury ameliorating effects[1][2][3][4][5][6][7][8][9][10][11].
IC50 & Target
Macrolide
Cellular Effect
Cell Line
Type
Value
Description
References
HeLa
IC50
160 μg/mL
Compound: Roxithromycin
Antiproliferative effect against HeLa cells after 48 hrs
Antiproliferative effect against HeLa cells after 48 hrs
Roxithromycin is active against various Gram-positive and Gram-negative bacteria, including five strains each of Staphylococcus and Streptococcus (geometric mean MICs = 0.08 and 0.79 µg/mL, respectively), as well as several strains each of Corynebacterium, Haemophilus, and S. pneumoniae (MIC50s = 0.02, 0.01, and 2.5 µg/mL, respectively)[5].
Roxithromycin (48 h) shows antiproliferative effect and inhibition of metabolic activity in HeLa (IC50 of 160 and 90 μg/mL, respectively), MG-63 (IC50 of 180 and 110 μg/mL, respectively) and Osteoblast cells (IC50 of 70 and 210 μg/mL, respectively)[1].
Roxithromycin (12.5-200 μM, 72 h) shows antiproliferative effect in HUVEC cells[2].
Roxithromycin (20-50 μM) inhibits endothelial cell migration and tube formation[6].
Roxithromycin (10 μM) inhibits chemokine-induced chemotaxis of Th1 and Th2 cells but regulatory T cells[7].
Roxithromycin (1-10 μM, 24 h) decreases ultraviolet B irradiation-induced reactive oxygen intermediates production and apoptosis of keratinocytes (SVHK cells)[8].
Roxithromycin (40-120 μM, 3 days) induces apoptosis to eliminate senescent cells (WI-38)[9].
Roxithromycin (10-80 μM, 24 h-72 h) inhibits senescent cell-induced fibroblast activation by inhibiting profibrotic SASP factors in MRC-5 cells[9].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Was resistant to UVB-induced cell death and the maximal inhibitory effect was detected at 1 μM
In Vivo
Roxithromycin (20 mg/kg, s.c. or p.o., single) is protective against infection by strains of S. aureus, S. pyogenes, S. pneumoniae, or L. monocytogenes in mice, with 50% protective dose (PD50) values ranging from 23 to 98 mg/kg[5].
Roxithromycin (40-100 mg/kg, i.p., twice daily) dose-dependently inhibits tumor angiogenesis in a mouse dorsal air sac model of angiogenesis, with reducing the dense capillary network area[6].
Roxithromycin (40-160 mg/kg, p.o., 16 days) attenuates Bleomycin (HY-108345)-induced lung injury, inflammation, and pulmonary fibrosis in mice[9].
Roxithromycin (40-100 mg/kg, i.p., thrice per week from week 10 to 17) inhibits constitutive activation of NF-κB by diminishing oxidative stress in a rat model of hepatocellular carcinoma[10].
Roxithromycin (5-40 mg/kg, i.p., 1 h) attenuates airway inflammation via MAPK/NF-κB activation in a mouse model of allergic asthma[11].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male C57BL/6 mice (received a single dose of BLM at 0.85 U/kg by intratracheal instillation)[9]
Dosage:
40, 80, 160 mg/kg
Administration:
oral gavage (p.o.), 16 days
Result:
Displayed a significantly lower lung/body weight ratio than the vehicle-treated mice.
Decreased the inflammatory cell numbers.
Reduced LDH, a useful indicator of lung tissue damage and inflammation in BALF.
Decreased dysfunction, presenting much more intact alveoli and thin, clear alveolar walls.
ameliorated the collagen deposition in a dose-dependent manner.
Decreased transcriptional levels of TGF-β, fibronectin, and collagen I.
Downregulated α-SMA expression.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (119.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.1947 mL
5.9734 mL
11.9467 mL
5 mM
0.2389 mL
1.1947 mL
2.3893 mL
10 mM
0.1195 mL
0.5973 mL
1.1947 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.99 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 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 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn 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.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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