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Roxithromycin

MCE China：Roxithromycin

Brand：MedChemExpress (MCE)

Cat. No.HY-B0435

CAS：80214-83-1

Synonyms：RU-28965

Purity：99.93%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Roxithromycin (RU-28965) is an orally active semi-synthethic macrolide antibiotic. 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.

In Vitro：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].

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].

IC50 & Target：Macrolide

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References：

[1]. Duewelhenke N, et al. Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines. Antimicrob Agents Chemother. 2007 Jan;51(1):54-63.  [Content Brief]

[2]. Takakusagi K, et al. Multimodal biopanning of T7 phage-displayed peptides reveals angiomotin as a potential receptor of the anti-angiogenic macrolide Roxithromycin. Eur J Med Chem. 2015 Jan 27;90:809-21.  [Content Brief]

[3]. Yamazaki H, et al. Comparative studies of in vitro inhibition of cytochrome P450 3A4-dependent testosterone 6beta-hydroxylation by roxithromycin and its metabolites, troleandomycin, and erythromycin. Drug Metab Dispos. 1998 Nov;26(11):1053-7.  [Content Brief]

[4]. Bertho G, et al. Transferred nuclear Overhauser effect study of macrolide-ribosome interactions: correlation between antibiotic activities and bound conformations. Bioorg Med Chem. 1998 Feb;6(2):209-21.  [Content Brief]

[5]. Chantot JF, et al. Antibacterial activity of roxithromycin: a laboratory evaluation. J Antibiot (Tokyo). 1986 May;39(5):660-8.  [Content Brief]

[6]. Yatsunami J, et al. Inhibition of tumor angiogenesis by roxithromycin, a 14-membered ring macrolide antibiotic. Cancer Lett. 1998 Sep 25;131(2):137-43.  [Content Brief]

[7]. Ito T, et al. Roxithromycin inhibits chemokine-induced chemotaxis of Th1 and Th2 cells but regulatory T cells. J Dermatol Sci. 2009 Jun;54(3):185-91.  [Content Brief]

[8]. Takahashi H, et al. Roxithromycin decreases ultraviolet B irradiation-induced reactive oxygen intermediates production and apoptosis of keratinocytes. J Dermatol Sci. 2004 Feb;34(1):25-33.  [Content Brief]

[9]. Zhang X, et al. Roxithromycin attenuates bleomycin-induced pulmonary fibrosis by targeting senescent cells. Acta Pharmacol Sin. 2021 Dec;42(12):2058-2068.  [Content Brief]

[10]. Ueno S, et al. Roxithromycin inhibits constitutive activation of nuclear factor {kappa}B by diminishing oxidative stress in a rat model of hepatocellular carcinoma. Clin Cancer Res. 2005 Aug 1;11(15):5645-50.  [Content Brief]

[11]. Ci X, et al. Short-term roxithromycin treatment attenuates airway inflammation via MAPK/NF-κB activation in a mouse model of allergic asthma. Inflamm Res. 2012 Jul;61(7):749-58.  [Content Brief]