Art. -Nr.: HY-17508

Clarithromycin

21 Cited Publications

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Based on 21 publication(s) in Google Scholar

Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.

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Reinheit: 99.90%
CAS. Nr.: 81103-11-9
Formel: C₃₈H₆₉NO₁₃
Molecular Weight:747.95

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Clarithromycin Chemical Structure

CAS. Nr.: 81103-11-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (21)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM^[2]. Clarithromycin significantly inhibits the HERG potassium current^[3].Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K^[4].

IC₅₀ & Target

CYP3

Macrolide

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
AML12	CC₅₀	>100 μM Compound: CLA	Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against mouse AML12 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38354519]
HFF	CC₅₀	260 μM Compound: 2	Cytotoxicity against HFF after 48 hrs by MTS assay Cytotoxicity against HFF after 48 hrs by MTS assay	[PMID: 21428405]
NIH-3T3-G185	IC₅₀	15.1 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	23.8 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	3.8 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	50.2 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	56.1 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	7.2 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	86.7 μM Compound: Clarithromycin	TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
THP-1	EC₅₀	0.046 mg/L Compound: Clarithromycin	Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 infected in human THP1 cells assessed as decrease of CFU after 24 hrs Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 25923 infected in human THP1 cells assessed as decrease of CFU after 24 hrs	[PMID: 19564365]

In Vitro

Clarithromycin produces a similar concentration-dependent block with an IC₅₀ of 45.7 μM^[3].
Clarithromycin induces the formation of numerous intracytoplasmic vacuoles after 24 h, in all cell lines, especially in HCT116 cells. Prolonged treatment with Clarithromycin (40, 80, and 160 μM) alters cell proliferation and triggers apoptotic cell death in colorectal cancer (CRC) cells. Inhibition of cell proliferation is potentiated when Clarithromycin is re-added to the cells. In particular, 160 μM Clarithromycin, re-added after 48 h of incubation, produces an arrest of cell proliferation at 72 h. Similar effects are obtained in LS174T cells^[4].
Clarithromycin (80 and 160 μM; 48 hours) strongly increases the LC3-II/LC3-I ratio, in a dose- and time-dependent manner, with a maximum at 24 h of treatment. This effect is accompanied by a decrease of p62/SQSTM1^[4].

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

Cell Proliferation Assay^[4]

Cell Line:

HCT116 cells
Concentration:

40, 80, and 160 µM
Incubation Time:

24, 48, 72 hours
Result:

Reduced HCT116 cell proliferation, although did not completely abolished it.

Western Blot Analysis^[4]

Cell Line:

HCT116 cells
Concentration:

80 and 160 µM
Incubation Time:

4, 24, 48 hours
Result:

A decrease of LC3-II and a re-increase of p62/SQSTM1 were observed at 48 hours treatment.

In Vivo

Clarithromycin at 200 mg/kg has activity against four tested in vivo^[5].

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

Animal Model:

Six-week-old beige (C57BL/6J bg^j/bg^j) mice which had been infected with viable M. avium ATCC 49601^[5]
Dosage:

50, 100, 200, or 300 mg/kg
Administration:

Administered daily by gavage
Result:

Reduced organ cell counts compared with those in mice given no treatment at all doses.
Had activity against three additional MAC isolates (MICs for the isolates ranged from 1 to 4 µg/mL by broth dilution) at 200 mg/kg.

Clinical Trial

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

Chemical Information

CAS. Nr. 81103-11-9
Appearance Solid
Molecular Weight 747.95
Formel C₃₈H₆₉NO₁₃
Color White to off-white
SMILES

C[C@@](OC)(C[C@H](C([C@@H]1C)=O)C)[C@@H]([C@H]([C@@H]([C@H](C(O[C@H](CC)[C@@](C)(O)[C@@H]1O)=O)C)O[C@@](O[C@@H](C)[C@@H]2O)([H])C[C@@]2(C)OC)C)O[C@@](O[C@H](C)C[C@@H]3N(C)C)([H])[C@@H]3O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (21)

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Journal Impact Factor

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
Water Res

Quantifying community-wide antibiotic usage via urban water fingerprinting: Focus on contrasting resource settings in South Africa. [Abstract]

2023 Jul 15:240:120110. PMID: 37247434
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
J Med Chem

Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]

2021 Mar 11;64(5):2725-2738. PMID: 33619967
J Clin Immunol

S100A4 Induces Neutrophilic Inflammation in Chronic Rhinosinusitis with Nasal Polyps via TLR4 Pathway. [Abstract]

2025 Nov 15;45(1):160. PMID: 41240201

Clarithromycin purchased from MedChemExpress. Usage Cited in: J Clin Immunol. 2025 Nov 15;45(1):160. [Abstract]

The mRNA expression levels of IL-6, IL-8 in hNECs stimulated by S100A4 with or without Clarithromycin (10 μM) and Dexamethasone .

Clarithromycin purchased from MedChemExpress. Usage Cited in: J Clin Immunol. 2025 Nov 15;45(1):160. [Abstract]

The protein expression levels of G-CSF, IL-36γ in hNECs stimulated by S100A4 with or without Clarithromycin (10 μM) and Dexamethasone.
Cell Prolif

Direct inhibitory effect on viral entry of influenza A and SARS-CoV-2 viruses by azithromycin. [Abstract]

2021 Jan;54(1):e12953. PMID: 33211371
J Chem Inf Model

Macrolides May Prevent Severe Acute Respiratory Syndrome Coronavirus 2 Entry into Cells: A Quantitative Structure Activity Relationship Study and Experimental Validation. [Abstract]

2021 Apr 26;61(4):2016-2025. PMID: 33734704
Eur J Pharm Sci

Investigating the relevance of CYP2J2 inhibition for drugs known to cause intermediate to high risk torsades de pointes. [Abstract]

2023 Aug 1:187:106475. PMID: 37225005
Antimicrob Agents Chemother

An enoyl-ACP reductase inhibitor, NITD-916, expresses anti- Mycobacterium abscessus activity. [Abstract]

2025 May 23:e0024925. PMID: 40407337
mLife

Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria. [Abstract]

2025 Apr 15;4(2):155-168. PMID: 40313980
Antimicrob Agents Chemother

TBAJ-587, a novel diarylquinoline, is active against Mycobacterium abscessus. [Abstract]

2024 Oct 29:e0094524. PMID: 39470202
Antimicrob Agents Chemother

Dihydrotanshinone I Is Effective against Drug-Resistant Helicobacter pylori In Vitro and In Vivo. [Abstract]

2021 Feb 17;65(3):e01921-20. PMID: 33318002
Front Microbiol

Tedizolid Activity Against Clinical Mycobacterium abscessus Complex Isolates-An in vitro Characterization Study. [Abstract]

2018 Sep 7:9:2095. PMID: 30245674
Microbiol Spectr

Antimicrobial resistance of rapidly growing mycobacteria isolated from companion animals in Taiwan. [Abstract]

2025 May 19:e0307424. PMID: 40387379
ACS Infect Dis

Toward a Bactericidal Oral Drug Combination for the Treatment of Mycobacterium abscessus Lung Disease. [Abstract]

2025 Apr 1. PMID: 40168319
ACS Chem Biol

Investigate Natural Product Indolmycin and the Synthetically Improved Analogue Toward Antimycobacterial Agents. [Abstract]

2022 Jan 21;17(1):39-53. PMID: 34908399
Pathogens

N-Acetylcysteine as a Host-Directed Therapy Against Clarithromycin-Resistant Mycobacterium abscessus. [Abstract]

2025 Mar 21;14(4):302. PMID: 40333083
Infect Drug Resist

In vitro Activity of the Novel Tetracyclines Derivative, Zifanocycline Against Mycobacterium abscessus. [Abstract]

2025 Oct 4:18:5239-5247. PMID: 41069760
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280
Authorea

2025 Sep 17.
bioRxiv

2024 Jan 18.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (44.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.3370 mL

6.6849 mL

13.3698 mL

5 mM

0.2674 mL

1.3370 mL

2.6740 mL

10 mM

0.1337 mL

0.6685 mL

1.3370 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(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 (3.34 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 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 (3.34 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 (3.34 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals 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 (286 KB)
SDS (393 KB)
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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]. D H Peters, et al. Clarithromycin. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic potential. Drugs. 1992 Jul;44(1):117-64. [Content Brief]

[2]. X J Zhao, et al. An in vitro study on the metabolism and possible drug interactions of rokitamycin, a macrolide antibiotic, using human liver microsomes. Drug Metab Dispos. 1999 Jul;27(7):776-85. [Content Brief]

[3]. Scott J C Stanat, et al. Characterization of the inhibitory effects of erythromycin and clarithromycin on the HERG potassium channel. Mol Cell Biochem. 2003 Dec;254(1-2):1-7. [Content Brief]

[4]. Giulia Petroni, et al. Clarithromycin inhibits autophagy in colorectal cancer by regulating the hERG1 potassium channel interaction with PI3K. Cell Death Dis. 2020 Mar 2;11(3):161. [Content Brief]

[5]. S P Klemens, et al. Activity of clarithromycin against Mycobacterium avium complex infection in beige mice. Antimicrob Agents Chemother. 1992 Nov;36(11):2413-7. [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, 6 months; -20°C, 1 month. 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
DMSO	1 mM	1.3370 mL	6.6849 mL	13.3698 mL	33.4245 mL
	5 mM	0.2674 mL	1.3370 mL	2.6740 mL	6.6849 mL
	10 mM	0.1337 mL	0.6685 mL	1.3370 mL	3.3425 mL
	15 mM	0.0891 mL	0.4457 mL	0.8913 mL	2.2283 mL
	20 mM	0.0668 mL	0.3342 mL	0.6685 mL	1.6712 mL
	25 mM	0.0535 mL	0.2674 mL	0.5348 mL	1.3370 mL
	30 mM	0.0446 mL	0.2228 mL	0.4457 mL	1.1142 mL
	40 mM	0.0334 mL	0.1671 mL	0.3342 mL	0.8356 mL

Keywords

Clarithromycin

21 Cited Publications

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Clarithromycin

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Publications Citing Use of MedChemExpress (MCE) Clarithromycin

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (21)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Clarithromycin Related Classifications

Art. -Nr.: HY-17508