Art. -Nr.: HY-B0435

Roxithromycin

(Synonyms: RU-28965)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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.

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Reinheit: 99.86%
CAS. Nr.: 80214-83-1
Formel: C₄₁H₇₆N₂O₁₅
Molecular Weight:837.05

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Roxithromycin Chemical Structure

CAS. Nr.: 80214-83-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Macrolide

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

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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	[PMID: 17088489]
HeLa	IC₅₀	90 μg/mL Compound: Roxithromycin	Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs	[PMID: 17088489]
HUVEC	IC₅₀	100 μM Compound: RXM	Inhibition of cell proliferation of HUVEC at 12.5 to 200 uM after 72 hrs by MTS assay Inhibition of cell proliferation of HUVEC at 12.5 to 200 uM after 72 hrs by MTS assay	[PMID: 25528335]
MG-63	IC₅₀	110 μg/mL Compound: Roxithromycin	Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs	[PMID: 17088489]
MG-63	IC₅₀	180 μg/mL Compound: Roxithromycin	Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs	[PMID: 17088489]
Osteoblast	IC₅₀	210 μg/mL Compound: Roxithromycin	Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs	[PMID: 17088489]
Osteoblast	IC₅₀	70 μg/mL Compound: Roxithromycin	Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs	[PMID: 17088489]

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].

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

Apoptosis Analysis^[1]

Cell Line:

SVHK cells following UVB-irradiation (30 mJ/cm²)
Concentration:

0.01, 0.1, 1, 10 μM
Incubation Time:

24 h
Result:

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 80214-83-1
Appearance Solid
Molecular Weight 837.05
Formel C₄₁H₇₆N₂O₁₅
Color White to off-white
SMILES

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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (7)

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Acta Pharm Sin B

Repurposing carrimycin as an antiviral agent against human coronaviruses, including the currently pandemic SARS-CoV-2. [Abstract]

2021 Sep;11(9):2850-2858. PMID: 33723501
Theranostics

Antibiotic Azithromycin inhibits brown/beige fat functionality and promotes obesity in human and rodents. [Abstract]

2022 Jan 1;12(3):1187-1203. PMID: 35154482
Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299
Emerg Contam

2026 Feb 23.
Water

2025 Jun 6.
bioRxiv

2026 Jan 14.
Ann Transl Med

Roxithromycin attenuates inflammation via modulation of RAGE-influenced calprotectin expression in a neutrophilic asthma model. [Abstract]

2021 Mar;9(6):494. PMID: 33850891

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (2.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO 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.

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 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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 μL DMSO stock solution (25.0 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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Portuguese - PT (458 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1947 mL	5.9734 mL	11.9467 mL	29.8668 mL
	5 mM	0.2389 mL	1.1947 mL	2.3893 mL	5.9734 mL
	10 mM	0.1195 mL	0.5973 mL	1.1947 mL	2.9867 mL
	15 mM	0.0796 mL	0.3982 mL	0.7964 mL	1.9911 mL
	20 mM	0.0597 mL	0.2987 mL	0.5973 mL	1.4933 mL
	25 mM	0.0478 mL	0.2389 mL	0.4779 mL	1.1947 mL
	30 mM	0.0398 mL	0.1991 mL	0.3982 mL	0.9956 mL
	40 mM	0.0299 mL	0.1493 mL	0.2987 mL	0.7467 mL
	50 mM	0.0239 mL	0.1195 mL	0.2389 mL	0.5973 mL
	60 mM	0.0199 mL	0.0996 mL	0.1991 mL	0.4978 mL
	80 mM	0.0149 mL	0.0747 mL	0.1493 mL	0.3733 mL
	100 mM	0.0119 mL	0.0597 mL	0.1195 mL	0.2987 mL

Keywords

Roxithromycin

7 Cited Publications

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Roxithromycin

Anti-Infection Compound Library

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Publications Citing Use of MedChemExpress (MCE) Roxithromycin

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Roxithromycin Related Classifications

Art. -Nr.: HY-B0435