2. Anti-infection Apoptosis Neuronal Signaling Membrane Transporter/Ion Channel
  3. Bacterial Antibiotic Apoptosis Calcium Channel
  4. Tilmicosin

Tilmicosin  (Synonyms: LY-177370; EL-870)

Cat. No.: HY-B0905 Purity: ≥98.0%
SDS COA Handling Instructions Technical Support

Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects.

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

Tilmicosin Chemical Structure

Tilmicosin Chemical Structure

CAS No. : 108050-54-0

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of Tilmicosin:

Tilmicosin Related Antibodies

Top Publications Citing Use of Products

View All Antibiotic Isoform Specific Products:

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

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Description

Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects[1][2][3][4][5][6].

IC50 & Target[3]

COX-2

 

In Vitro

Tilmicosin (0-7 μg/mL; 16-18 h) has the MIC for 90% of Staphylococcus aureus isolates from the bovine udder of 0.78 μg/mL[1].
Tilmicosin (0.5μg /mL; 2 h) induces apoptosis of bovine neutrophils[2].
Tilmicosin (5-20 μg/mL; 18 h) inhibits the expression of COX-2 and iNOS in LPS (HY-D1056) treated macrophages, and affects the secretion of cytokines[3].

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

Tilmicosin Related Antibodies

RT-PCR[3]

Cell Line: LPS (HY-D1056) treated RAW264.7 cells
Concentration: 5, 10 and 20 μg/mL
Incubation Time: 18 h
Result: Reduced the levels of COX-2 and iNOS.
In Vivo

Tilmicosin (75 mg/kg; subcutaneous injection; single dose) induces cardiotoxicity in mice[4].
Pharmacokinetic Analysis in lung tissues of the M. gallisepticum infected chickens[5]

Route Dose (mg/kg) t1/2kel (h) Tmax (h) Cmax (μg/g) AUC (μg·h/g) MRT (h) CL/F (1/h/kg)
p.o. 1 48.46 12.00 0.12 13.62 53.60 0.09
p.o. 30 50.60 12.00 6.19 464.23 50.88 0.06

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

Animal Model: Male albino mice[4]
Dosage: 75 mg/kg
Administration: Subcutaneous injection (s.c.); single dose
Result: Significantly increased cardiac injury markers in serum (LDH, CK and CK-MB).
Significantly increased the cardiac MDA content and decreased cardiac GSH, SOD, CAT and TAC.
Molecular Weight

869.13

Formula

C46H80N2O13
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]([C@@H](CC1=O)O)[C@H]([C@H](C[C@H](C(/C=C/C(C)=C/[C@H](CO[C@H](O[C@H](C)[C@@H](O)[C@H]2OC)[C@@H]2OC)[C@@H](CC)O1)=O)C)CCN(C[C@H](C)C3)C[C@H]3C)O[C@@](O[C@H](C)[C@@H](O)[C@@H]4N(C)C)([H])[C@@H]4O
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: 

1M HCl : 100 mg/mL (115.06 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 100 mg/mL (115.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1506 mL 5.7529 mL 11.5058 mL
5 mM 0.2301 mL 1.1506 mL 2.3012 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
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Concentration
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Volume
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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 (2.88 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 (2.88 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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: ≥98.0%

SDS (597 KB)

COA (252 KB) HNMR (351 KB) MS (214 KB)

Handling Instructions (2659 KB)
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
1M HCl / DMSO 1 mM 1.1506 mL 5.7529 mL 11.5058 mL 28.7644 mL
5 mM 0.2301 mL 1.1506 mL 2.3012 mL 5.7529 mL
10 mM 0.1151 mL 0.5753 mL 1.1506 mL 2.8764 mL
15 mM 0.0767 mL 0.3835 mL 0.7671 mL 1.9176 mL
20 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
25 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1506 mL
30 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
40 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
50 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
60 mM 0.0192 mL 0.0959 mL 0.1918 mL 0.4794 mL
80 mM 0.0144 mL 0.0719 mL 0.1438 mL 0.3596 mL
100 mM 0.0115 mL 0.0575 mL 0.1151 mL 0.2876 mL
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Tilmicosin 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.

Keywords:

Tilmicosin108050-54-0LY-177370 EL-870LY177370LY 177370EL870EL 870EL-870BacterialAntibioticApoptosisCalcium ChannelCa2+ channelsCa channelsneutrophilsmacrophagesInhibitorinhibitorinhibit

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