Clarithromycin(Synonyms: 克拉霉素)

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Clarithromycin (Synonyms: 克拉霉素) 纯度: ≥98.0%

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)。

Clarithromycin(Synonyms: 克拉霉素)

Clarithromycin Chemical Structure

CAS No. : 81103-11-9

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生物活性

Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) 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].

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(In Vivo)

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old beige (C57BL/6J bgj/bgj) 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

分子量

747.95

Formula

C38H69NO13

CAS 号

81103-11-9

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
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (44.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

    [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.

    [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.

    [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.

    [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.

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