Clarithromycin 具有广谱的抗菌 (antimicrobial) 活性。Clarithromycin 抑制CYP3A4催化的三唑仑 α-羟基化，IC50(Ki) 值为 56 (43) μM。Clarithromycin 抑制 HERG 钾电流。Clarithromycin 通过削弱连接 hERG1 和 PI3K 的信号通路来影响自噬流 (autophagic flux)。
| 生物活性 | Clarithromycin has a broad spectrum ofantimicrobialactivity. Clarithromycin inhibits theCYP3A4-catalyzed triazolam alpha-hydroxylation with theIC50(Ki) value of 56 (43) μM[2]. Clarithromycin significantly inhibits theHERG potassium current[3].Clarithromycin affects theautophagic fluxby impairing the signaling pathway linking hERG1 andPI3K[4]. |
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体外研究
(In Vitro) | Clarithromycin produces a similar concentration-dependent block with an IC50of 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].
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. |
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体内研究
(In Vivo) | Clarithromycin at 200 mg/kg has activity against four tested in vivo[5].
| Animal Model: | Six-week-old beige (C57BL/6J bgj/bgj) mice which had been infected with viableM. aviumATCC 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. |
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| 中文名称 | 克拉霉素；克拉红霉素；6-0-甲基红霉素A；6氧甲基红霉素；甲红霉素；甲氧基红霉素；克红霉素 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(44.56 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3370 mL | 6.6849 mL | 13.3699 mL | | 5 mM | 0.2674 mL | 1.3370 mL | 2.6740 mL | | 10 mM | 0.1337 mL | 0.6685 mL | 1.3370 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (3.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (3.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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