テリスロマイシン
Based on 5 publication(s) in Google Scholar
Telithromycin (HMR3647) is a novel ketolide antibiotic that structurally resembles macrolides. Telithromycin belongs to the ketolide family that is characterized by a keto group at position 3 of the macrolide ring and is active against bacteria causing community-acquired pneumonia, acute exacerbation of chronic bronchitis, and acute sinusitis. Telithromycin also has similar immunomodulatory effects as macrolides. Telithromycin can be used for the research of respiratory infections including bronchial asthma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.96%
- CAS 番号: 191114-48-4
- 分子式: C43H65N5O10
- 分子量:812.00
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Telithromycin
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生物活性
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Macrolide |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AML12 | CC50 |
>100 μM
Compound: TEL
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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
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[PMID: 38354519] |
| TE-671 | IC50 |
3.5 μM
Compound: Telithromycin
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Inhibition of human nAChR expressed in human TE671 cells assessed as reduction in nicotine-induced current response by whole-cell patch-clamp method
Inhibition of human nAChR expressed in human TE671 cells assessed as reduction in nicotine-induced current response by whole-cell patch-clamp method
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[PMID: 31644280] |
| THP-1 | EC50 |
0.11 mg/L
Compound: Telithromycin
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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
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[PMID: 19564365] |
Telithromycin (HMR3647) (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced MUC5AC production[1].
Telithromycin (0-50 μg/mL, 30 min) suppress C. pneumoniae-induced NF-kB activation[1].
Telithromycin (10 mg/mL, 1 h) inhibits the production of MIP-2 and TNF-α in a dose-dependent manner by LPS-stimulated RAW 264.7 macrophages[2].
Telithromycin (10 mg/mL, 1 h) inhibits NF-kB activation, increases apoptosis in cell and decreases the LPS-induced influx of neutrophils in BAL fluid[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H292 cells
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Concentration:0-50 μg/mL
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Incubation Time:30 min
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Result:Suppressed C. pneumoniae-induced MUC5AC production in dose-dependently and significantly decreased MUC5AC production at 50 mg/mL.
Suppressed p65 and p50 activation in NCI-H292 cells.
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Cell Line:RAW 264.7 and MLE-12 cells
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Concentration:10 mg/mL
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Incubation Time:1 h
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Result:Increased the apoptotic activity in cells induced with supernatants from LPS-treated RAW 264.7 macrophages and in LPS-induced cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-Nebulized Mice[2]
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Dosage:20 mg/kg
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Administration:20 mg/kg, ip., single
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Result:Increased the protein concentration, reduced the concentrations of nitrite and the levels of TNF-α and induced significant reductions the levels of MIP-2.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 191114-48-4
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性状 Solid
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分子量 812.00
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分子式 C43H65N5O10
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Color White to off-white
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SMILES
O[C@H]1[C@]([H])(O[C@@H]([C@](C)(OC)C[C@@H](C)C2=O)[C@@H](C)C([C@@H](C)C(O[C@H](CC)[C@](OC(N3CCCCN4C=C(C5=CC=CN=C5)N=C4)=O)(C)[C@@]3([H])[C@H]2C)=O)=O)O[C@H](C)C[C@@H]1N(C)C
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別名
Telithromycin; HMR3647; RU66647
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Theranostics
Antibiotic Azithromycin inhibits brown/beige fat functionality and promotes obesity in human and rodents. [Abstract]2022 Jan 1;12(3):1187-1203. PMID: 35154482 -
Mol Cell Proteomics
Common Metabolic Pathways Implicated in Resistance to Chemotherapy Point to a Key Mitochondrial Role in Breast Cancer. [Abstract]2019 Feb;18(2):231-244. PMID: 30373788 -
Microb Biotechnol
Attenuator LRR - a regulatory tool for modulating gene expression in Gram-positive bacteria. [Abstract]2021 Nov;14(6):2538-2551. PMID: 33720523 -
BMC Microbiol
The antimicrobial activity of cethromycin against Staphylococcus aureus and compared with erythromycin and telithromycin. [Abstract]2023 Apr 20;23(1):109. PMID: 37081393 -
溶剤 & 溶解度
DMSO : ≥ 90 mg/mL (110.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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- Portuguese - PT (478 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yoshitomo Morinaga, et al. Azithromycin, clarithromycin and telithromycin inhibit MUC5AC induction by Chlamydophila pneumoniae in airway epithelial cells. Pulm Pharmacol Ther. 2009 Dec;22(6):580-6. [Content Brief]
[2]. Magdalena Leiva, et al. Effects of telithromycin in in vitro and in vivo models of lipopolysaccharide-induced airway inflammation. Chest. 2008 Jul;134(1):20-9. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2315 mL | 6.1576 mL | 12.3153 mL | 30.7882 mL |
| 5 mM | 0.2463 mL | 1.2315 mL | 2.4631 mL | 6.1576 mL | |
| 10 mM | 0.1232 mL | 0.6158 mL | 1.2315 mL | 3.0788 mL | |
| 15 mM | 0.0821 mL | 0.4105 mL | 0.8210 mL | 2.0525 mL | |
| 20 mM | 0.0616 mL | 0.3079 mL | 0.6158 mL | 1.5394 mL | |
| 25 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2315 mL | |
| 30 mM | 0.0411 mL | 0.2053 mL | 0.4105 mL | 1.0263 mL | |
| 40 mM | 0.0308 mL | 0.1539 mL | 0.3079 mL | 0.7697 mL | |
| 50 mM | 0.0246 mL | 0.1232 mL | 0.2463 mL | 0.6158 mL | |
| 60 mM | 0.0205 mL | 0.1026 mL | 0.2053 mL | 0.5131 mL | |
| 80 mM | 0.0154 mL | 0.0770 mL | 0.1539 mL | 0.3849 mL | |
| 100 mM | 0.0123 mL | 0.0616 mL | 0.1232 mL | 0.3079 mL |
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