1. Anti-infection
  2. Bacterial Antibiotic
  3. Telithromycin

Telithromycin  (Synonyms: HMR3647; RU66647)

Cat. No.: HY-A0062 Purity: 99.34%
SDS COA Handling Instructions

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.

For research use only. We do not sell to patients.

Telithromycin Chemical Structure

Telithromycin Chemical Structure

CAS No. : 191114-48-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 215 In-stock
25 mg USD 495 In-stock
50 mg USD 800 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Telithromycin:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

Macrolide

 

Cellular Effect
Cell Line Type Value Description References
TE-671 IC50
3.5 μM
Compound: Telithromycin
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
[PMID: 31644280]
THP-1 EC50
0.11 mg/L
Compound: Telithromycin
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
[PMID: 19564365]
In Vitro

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.

RT-PCR[1]

Cell Line: NCI-H292 cells
Concentration: 0-50 μg/mL
Incubation Time: 30 min
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.

Apoptosis Analysis[2]

Cell Line: RAW 264.7 and MLE-12 cells
Concentration: 10 mg/mL
Incubation Time: 1 h
Result: Increased the apoptotic activity in cells induced with supernatants from LPS-treated RAW 264.7 macrophages and in LPS-induced cells.
In Vivo

Telithromycin (HMR3647) (20 mg/kg, ip., single) reduces protein, nitrite, MIP-2, and TNF-α levels in the BAL fluid of LPS-nebulized animals[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LPS-Nebulized Mice[2]
Dosage: 20 mg/kg
Administration: 20 mg/kg, ip., single
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.
Clinical Trial
Molecular Weight

812.00

Formula

C43H65N5O10

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2315 mL 6.1576 mL 12.3153 mL
5 mM 0.2463 mL 1.2315 mL 2.4631 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.71%

References

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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Telithromycin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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