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Chemical Structure| 80214-83-1 Chemical Structure| 80214-83-1

Structure of Roxithromycin
CAS No.: 80214-83-1

Chemical Structure| 80214-83-1

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Roxithromycin is a bacteriostatic drug acts by inhibiting protein synthesis through binding reversibly to 50S ribosomal subunits of sensitive microorganism.

Synonyms: RU-28965; RU 965; Rulide

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Product Details of Roxithromycin

CAS No. :80214-83-1
Formula : C41H76N2O15
M.W : 837.05
SMILES Code : C[C@H]([C@H]([C@](O)(C[C@H](/C1=N\OCOCCOC)C)C)O[C@@](O[C@H](C)C[C@@H]2N(C)C)([H])[C@@H]2O)[C@]([C@H](C(O[C@@H]([C@@](O)([C@H](O)[C@H]1C)C)CC)=O)C)([H])O[C@@](O[C@@H](C)[C@@H]3O)([H])C[C@@]3(C)OC
Synonyms :
RU-28965; RU 965; Rulide
MDL No. :MFCD00214389

Safety of Roxithromycin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MRC-5 cells 10, 20, 40, 80 μM 24 h Evaluate the effect of roxithromycin on TGF-β-induced fibroblast activation, results showed that roxithromycin dose-dependently inhibited the expression of fibronectin, collagen I and α-SMA PMC8633281
A549 cells 40, 80 μM 24 h Evaluate the effect of roxithromycin on BLM-induced cell cycle arrest, results showed that roxithromycin significantly suppressed the expression of p53, p21, and p16 PMC8633281
WI-38 cells 20, 40, 60, 80, 100 μM 60–72 h Evaluate the killing effect of roxithromycin on senescent cells, results showed that roxithromycin selectively killed senescent cells PMC8633281
Rat airway smooth muscle cells 100 μg/ml 48 h To investigate the inhibitory effect of roxithromycin on TGF-β1-induced ASMCs proliferation and its mechanism, results showed that roxithromycin significantly inhibited ASMCs proliferation and up-regulated caveolin-1 expression PMC4256937
Streptococcus pneumoniae NMU112 0.5 to 5 μg/ml 12 h To evaluate the effect of roxithromycin on the production of pneumococcal virulence factors (PLY and PspA). Results showed that roxithromycin did not suppress the production of PLY and PspA at sub-MIC levels. PMC1855574
Human monocyte-derived macrophages 10 μg/ml 7 days Evaluate the intracellular bactericidal activity of roxithromycin against three clinical isolates of M. avium (MO-1, N-92159, and N-93043). Results showed that roxithromycin was bactericidal for strains MO-1 and N-92159 and bacteriostatic for strain N-93043. Compared with clarithromycin, the intracellular activities of roxithromycin were not significantly different after 7 days of treatment PMC162646
Freshly isolated rat hepatocytes 5 mg/L 5, 10, 20, 30, 60, and 120 min To study the uptake kinetics of roxithromycin and erythromycin base, results showed that the uptake of roxithromycin was about 1.8 to 2.5 times that of erythromycin base. PMC175915

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 male mice Bleomycin-induced pulmonary fibrosis model Oral gavage 40, 80, 160 mg/kg Once daily for 3 weeks Evaluate the effect of roxithromycin on bleomycin-induced pulmonary fibrosis, results showed that roxithromycin attenuated lung injury, inflammation, and fibrosis PMC8633281
Beige mice Disseminated Mycobacterium avium complex infection model Gavage 200 mg/kg Once daily for 28 days Roxithromycin alone significantly reduced the bacterial load of Mycobacterium avium complex in the blood, liver, and spleen of beige mice and decreased mortality. The combination of roxithromycin with ethambutol showed enhanced antibacterial effects in splenic tissues compared to roxithromycin alone. PMC163255
CBA/J mice Pneumonia model Oral gavage 1.25 to 10 mg/kg Twice daily for 3 days To evaluate the effect of roxithromycin on host resistance against macrolide-resistant S. pneumoniae infection. Results showed that roxithromycin (≥5 mg/kg/day) increased the median survival time and delayed bacteremia without suppressing the production of PLY and PspA in infected lungs. PMC1855574
C57BL/6 mice M. avium MO-1 infection model Oral gavage 200 mg/kg 6 days per week for 16 weeks Evaluate the efficacy of roxithromycin against M. avium MO-1 infection in C57BL/6 mice. Results showed that both roxithromycin and clarithromycin significantly reduced bacterial loads in spleens and lungs. Clarithromycin was more effective than roxithromycin in lungs, while their activities were comparable in spleens. No resistant mutants were selected during the 16-week treatment period PMC162646

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02735707 Community-Acquired Pneumonia Phase 4 Recruiting June 2022 -
NCT03571230 Helicobacter Pylori Infection ... More >> Antimicrobial Susceptibility Testing Less << Phase 4 Not yet recruiting January 30, 2020 China, Shandong ... More >> Xiuli Zuo Not yet recruiting Jinan, Shandong, China Contact: Xiuli Zuo, PhD,MD    15588818685 ext 053188369277    zuoxiuli@sina.com    Sub-Investigator: Jing Liu, MD          Sub-Investigator: Chaoran Ji, MD Less <<
NCT02819570 Premature Rupture of Membrane Phase 4 Unknown December 2017 Israel ... More >> Galil Medical Center Recruiting Nahariyya, Israel Contact: Maya Wolf, MD    972-507887800    homesickid@yahoo.com Less <<
NCT02469298 Virus Diseases Phase 2 Completed - -
NCT00285493 Low Back Pain Phase 1 Withdrawn(Withdrawn study halt... More >>ed prematurely, prior to enrollment of first participant) Less << - -
NCT03148444 Infection, Bacterial ... More >> Pacemaker Complication Less << Phase 4 Not yet recruiting June 1, 2020 -
NCT02469298 - Completed - -
NCT01843946 - Completed - Korea, Republic of ... More >> The Catholic University of Korea, St. Vincent's Hospital Suwon, Korea, Republic of, 442-723 Less <<
NCT03414918 Hyperaldosteronism Not Applicable Not yet recruiting January 2020 Italy ... More >> Department of Medicine - DIMED, University of Padova, Italy Not yet recruiting Padova, Italy Principal Investigator: Gian Paolo Rossi, MD Less <<
NCT00621387 Reactive Arthritis Not Applicable Completed - Finland ... More >> Division of Rheumatology, Department of Medicine Helsinki, Finland, 00029 Peijas Hospital Vantaa, Finland, 01400 Less <<
NCT00197379 Alopecia Not Applicable Unknown January 2007 Japan ... More >> Department of Dermatology, Hamamatsu University School of Medicine Hamamatsu, Japan, 431-3192 Less <<
NCT03565484 Helicobacter Pylori Infection Phase 4 Not yet recruiting April 30, 2020 China, Shandong ... More >> Qilu hosipital Not yet recruiting Jinan, Shandong, China, 257000 Contact: Xiuli Zuo, MD,PhD    15588818685 ext 053188369277    zuoxiuli@sina.com    Sub-Investigator: Chaoran Ji, MD          Sub-Investigator: Jing Liu, MD Less <<
NCT00439062 Rheumatoid Arthritis PHASE4 COMPLETED 2025-06-06 Nazilli State Hospital, Nazill... More >>i, Aydin, 09800, Turkey Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.19mL

0.24mL

0.12mL

5.97mL

1.19mL

0.60mL

11.95mL

2.39mL

1.19mL

References

 

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