Clarithromycin

製品コードS2555 バッチS255503

印刷

化学情報

Synonyms

A-56268

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₈H₆₉NO₁₃

分子量

747.95

CAS No.

81103-11-9

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

50 mg/mL (66.84 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3mg/ml (4.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
in vitro	Clarithromycin suppresses this production in a dose-dependent manner in both monocytes and THP-1 cells. This compound regulates three other promoters that have either the NF-kappa B or the AP-1 binding sequences: two synthetic (pAP-1-Luc and pNF-kappa B-Luc) and one naturally occurring (ELAM-Luc). ^[1] It suppresses NF-kappaB activation induced by TNF-alpha in U-937 and Jurkat cells in a concentration-related manner. The chemical inhibits NF-kappaB activation induced by TNF-alpha in U-937, Jurkat, and A549 cells and PBMC and by SEA in PBMC. It prevents NF-kappaB-dependent reporter gene expression in U-937 cells. ^[2] This agent results in a significant suppression of production of each cytokine in 71% and a significant increase in 29% of the human monocytes. ^[3] It inhibits tumor necrosis factor (TNF)-alpha-induced IL-8 gene expression in a dose- and incubation time-dependent manner. This compound represses AP-1 binding in TNF-alpha-treated BET-1A cells. It represses IL-8 gene transcription mainly via the AP-1 binding site in human bronchial epithelial cells. ^[4] The substance suppresses IL-1 beta gene expression in human nasal epithelial cells stimulated by H. influenzae endotoxin (HIE). It suppresses intercellular adhesion molecule-1 gene expression in nasal fibroblasts stimulated by IL-1 beta. This chemical reduces DNA-binding activity of NF-kappa B in both human nasal epithelial cells and fibroblasts stimulated by HIE or IL-1 beta, respectively. ^[5]

製品説明

Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.

in vitro

Clarithromycin suppresses this production in a dose-dependent manner in both monocytes and THP-1 cells. This compound regulates three other promoters that have either the NF-kappa B or the AP-1 binding sequences: two synthetic (pAP-1-Luc and pNF-kappa B-Luc) and one naturally occurring (ELAM-Luc). ^[1] It suppresses NF-kappaB activation induced by TNF-alpha in U-937 and Jurkat cells in a concentration-related manner. The chemical inhibits NF-kappaB activation induced by TNF-alpha in U-937, Jurkat, and A549 cells and PBMC and by SEA in PBMC. It prevents NF-kappaB-dependent reporter gene expression in U-937 cells. ^[2] This agent results in a significant suppression of production of each cytokine in 71% and a significant increase in 29% of the human monocytes. ^[3] It inhibits tumor necrosis factor (TNF)-alpha-induced IL-8 gene expression in a dose- and incubation time-dependent manner. This compound represses AP-1 binding in TNF-alpha-treated BET-1A cells. It represses IL-8 gene transcription mainly via the AP-1 binding site in human bronchial epithelial cells. ^[4] The substance suppresses IL-1 beta gene expression in human nasal epithelial cells stimulated by H. influenzae endotoxin (HIE). It suppresses intercellular adhesion molecule-1 gene expression in nasal fibroblasts stimulated by IL-1 beta. This chemical reduces DNA-binding activity of NF-kappa B in both human nasal epithelial cells and fibroblasts stimulated by HIE or IL-1 beta, respectively. ^[5]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/12003967/
https://pubmed.ncbi.nlm.nih.gov/11120942/
https://pubmed.ncbi.nlm.nih.gov/10221415/

https://pubmed.ncbi.nlm.nih.gov/10615065/
https://pubmed.ncbi.nlm.nih.gov/10646728/

+ 展开

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CAVIN1-Mediated hERG Dynamics: A Novel Mechanism Underlying the Interindividual Variability in Drug-Induced Long QT [ Circulation, 2024, 150(7):563-576]	PubMed: 38682330
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421]	PubMed: 35889140
Integrated lipidomic and transcriptomic analysis reveals clarithromycin-induced alteration of glycerophospholipid metabolism in the cerebral cortex of mice [ Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5]	PubMed: 34458952
Clarithromycin synergizes with cisplatin to inhibit ovarian cancer growth in vitro and in vivo. [ J Ovarian Res, 2019, 12(1):107]	PubMed: 31703731
Impact of Dynamically Exposed Polarity on Permeability and Solubility of Chameleonic Drugs Beyond the Rule of 5. [ J Med Chem, 2018, 61(9):4189-4202]	PubMed: 29608068
Twenty-seven-nucleotide repeat insertion in the rplV gene confers specific resistance to macrolide antibiotics in Staphylococcus aureus [ Oncotarget, 2018, 9(40):26086-26095]	PubMed: 29899844

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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