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Clarithromycin/克拉霉素

货号:A155509 同义名: 克拉红霉素;6氧甲基红霉素 / A-56268; TE 031

Clarithromycin是一种大环内酯类抗生素,抑制 CYP3A4 催化的三唑仑 α-羟基化,IC50 (Ki) 为 56 (43) μM,并具有抗菌和抗自噬活性。

Clarithromycin/克拉霉素 化学结构 CAS号:81103-11-9
Clarithromycin/克拉霉素 化学结构
CAS号:81103-11-9
Clarithromycin/克拉霉素 3D分子结构
CAS号:81103-11-9
Clarithromycin/克拉霉素 化学结构 CAS号:81103-11-9
Clarithromycin/克拉霉素 3D分子结构 CAS号:81103-11-9
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Clarithromycin/克拉霉素 纯度/质量文件 产品仅供科研

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Clarithromycin/克拉霉素 生物活性

描述 Clarithromycin exhibits a wide range of antimicrobial effects and is known for its capability to inhibit the CYP3A4 enzyme, which catalyzes the alpha-hydroxylation of triazolam, demonstrating an IC50 (Ki) value of 56 (43) µM[1]. This antibiotic also significantly blocks the HERG potassium current in a concentration-dependent manner, with an IC50 of 45.7 µM[2]. Clarithromycin impacts autophagic flux by disrupting the signaling pathway that connects hERG1 and PI3K[3].
体内研究

Additionally, Clarithromycin at a dose of 200 mg/kg exhibits efficacy against four in vivo tested pathogens[5], further highlighting its broad-spectrum antimicrobial activity[4].

体外研究

In various cell lines, especially HCT116 cells, Clarithromycin prompts the formation of numerous intracytoplasmic vacuoles after 24 hours. Extended treatment with Clarithromycin at concentrations of 40, 80, and 160 µM not only affects cell proliferation but also induces apoptotic cell death in colorectal cancer (CRC) cells. The inhibition of cell proliferation is enhanced when Clarithromycin is reapplied to the cells after initial treatment. For instance, reapplication of 160 µM Clarithromycin following a 48-hour incubation period leads to a halt in cell proliferation at 72 hours, with similar outcomes observed in LS174T cells[3].

Moreover, Clarithromycin significantly elevates the LC3-II/LC3-I ratio in a dose- and time-dependent fashion, reaching a peak at 24 hours of treatment. This increase in autophagic markers is also marked by a reduction in p62/SQSTM1 levels, indicating autophagy activation[3].

Clarithromycin/克拉霉素 细胞实验

Cell Line
Concentration Treated Time Description References
Mtb H37Rv strain 8 μM 5 days Evaluate the inhibitory activity of clarithromycin against Mtb H37Rv strain. Results showed an MIC of 8 μM for clarithromycin. Cell. 2023 Mar 2;186(5):1013-1025.e24.
Helicobacter pylori 0-16 μg/mL 24 hours To evaluate the in vitro bactericidal activity of CLR-loaded Mg-based micromotors against H. pylori, showing comparable bactericidal activity to free CLR solution. Nat Commun. 2017 Aug 16;8(1):272.
Peripheral blood mononuclear cells (PBMC) 100 μM 30 minutes To evaluate the effect of clarithromycin on corticosteroid sensitivity in PBMCs from COPD patients. Clarithromycin at 100 μM partially restored corticosteroid sensitivity. Br J Pharmacol. 2013 Jul;169(5):1024-34.
Human sinonasal epithelial cells 10, 50, 100 μM 12, 24, 36 hours To evaluate the effect of clarithromycin on the expression of 11β-HSD1, 3β-HSD, CYP21, and CYP11B1 in human sinonasal epithelial cells. Results showed that clarithromycin increased the expression of these enzymes in a dose- and time-dependent manner and enhanced cortisol production. Br J Pharmacol. 2015 Nov;172(21):5083-95.

Clarithromycin/克拉霉素 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice H. pylori infection model Oral 64 μg/kg Once a day for 5 consecutive days To evaluate the in vivo efficacy of RHL/Cl-Ch-cal in H. pylori-infected mice model Acta Pharm Sin B. 2022 Sep;12(9):3498-3512
Mice H. pylori infection model Oral gavage 30 mg/kg Once daily for five consecutive days To assess the therapeutic efficacy of CLR-loaded Mg-based micromotors in vivo against H. pylori infection, showing significant reduction in bacterial burden in the stomach. Nat Commun. 2017 Aug 16;8(1):272.
BALB/c mice Murine model of Buruli ulcer Oral 100 mg/kg Daily administration for 8 weeks Evaluated the efficacy of clarithromycin in combination with rifampin for treating Buruli ulcer, showing effectiveness but with gastrointestinal tolerability issues Acta Pharm Sin B. 2021 Mar;11(3):738-749
Mice Thigh infection model and bacteremia model Intraperitoneal and oral 200 mg/kg Single dose (thigh infection model) or daily for 5 days (bacteremia model) Clarithromycin and colistin combination therapy showed significant efficacy against mcr-1-positive K. pneumoniae infection at clinically relevant doses Nat Commun. 2018 Jan 31;9(1):458.
INS-GAS mice H. pylori infection model Oral 7.15 mg/kg/d Twice daily for 7 days To evaluate the efficacy of clarithromycin in combination with omeprazole and metronidazole in eradicating H. pylori infection and its impact on gastric cancer development in INS-GAS mice. Results showed that eradication therapy at 8, 12, or 22 WPI significantly reduced the severity of dysplasia and completely prevented GIN development when administered at 8 WPI. Cancer Res. 2008 May 1;68(9):3540-8
Balb/c mice Adrenalectomy model Intraperitoneal injection 100 mg/kg Once daily for 7 days To assess the effect of clarithromycin on the expression of steroid-synthesizing and steroid-converting enzymes in mouse nasal mucosa. Results showed that clarithromycin upregulated the expression of 3β-HSD, CYP11A1, CYP21, CYP11B1, and 11β-HSD1, but this effect was not observed in adrenalectomized mice. Br J Pharmacol. 2015 Nov;172(21):5083-95.
Mice P27-deficient mouse model Oral 7.15 mg/kg/day Twice daily for seven days To evaluate the therapeutic effect of clarithromycin in combination with omeprazole and metronidazole on H. pylori infection, showing significant reduction in gastric inflammation and premalignant lesions in treated groups Cancer Lett. 2014 Dec 1;355(1):106-12

Clarithromycin/克拉霉素 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01159574 Multiple Myeloma Phase 2 Active, not recruiting June 2020 United States, New York ... 展开 >> Weill Cornell Medical College New York, New York, United States, 10065 收起 <<
NCT03487562 Healthy Phase 1 Recruiting August 29, 2018 Korea, Republic of ... 展开 >> Seoul National University Hospital Recruiting Seoul, Korea, Republic of Contact: In-Jin Jang, MD, PhD    82-2-2072-1666    ijjang@snu.ac.kr    Principal Investigator: In-Jin Jang, MD, PhD 收起 <<
NCT01559935 - Active, not recruiting - -

Clarithromycin/克拉霉素 参考文献

[1]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.

[2]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.

[3]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.

[4]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.

Clarithromycin/克拉霉素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.34mL

0.27mL

0.13mL

6.68mL

1.34mL

0.67mL

13.37mL

2.67mL

1.34mL

Clarithromycin/克拉霉素 技术信息

CAS号81103-11-9
分子式C38H69NO13
分子量 747.95
SMILES Code C[C@@](C[C@@H](C)C([C@@H]1C)=O)([C@H](O[C@@]([H])([C@@H]2O)O[C@@H](C[C@@H]2N(C)C)C)[C@@H](C)[C@H](O[C@@]([H])(C[C@]3(OC)C)O[C@H]([C@@H]3O)C)[C@@H](C)C(O[C@@H]([C@@](O)([C@@H]1O)C)CC)=O)OC
MDL No. MFCD00865140
别名 克拉红霉素;6氧甲基红霉素;6-0-甲基红霉素A;甲红霉素;甲氧基红霉素;克红霉素 ;A-56268; TE 031; Antibiotic A 56268
运输蓝冰
InChI Key AGOYDEPGAOXOCK-KCBOHYOISA-N
Pubchem ID 84029
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 35 mg/mL(46.79 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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