Art. -Nr.: HY-B0905A

Tilmicosin phosphate

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

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

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

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Reinheit: 98.0%
CAS. Nr.: 137330-13-3
Formel: C₄₆H₈₃N₂O₁₇P
Molecular Weight:967.13

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Tilmicosin phosphate Chemical Structure

CAS. Nr.: 137330-13-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[3]

COX-2

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle NO Synthase Isoform-spezifische Produkte anzeigen :

Alle COX Isoform-spezifische Produkte anzeigen :

In Vitro

Non-salt dose:
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.

RT-PCR^[3]

Cell Line:

LPS (HY-D1056) treated RAW264.7 cells
Concentration:

5, 10 and 20 μg/mL (Non-salt dose)
Incubation Time:

18 h
Result:

Reduced the levels of COX-2 and iNOS.

In Vivo

Non-salt dose:
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)	t_1/2kel (h)	T_max (h)	C_max (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 (Non-salt dose)
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.

Chemical Information

CAS. Nr. 137330-13-3
Appearance Solid
Molecular Weight 967.13
Formel C₄₆H₈₃N₂O₁₇P
Color Light yellow to yellow
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.O=P(O)(O)O
Synonyms

LY-177370 phosphate; EL-870 phosphate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (5)

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Journal Impact Factor

Pak Vet J

2026 Feb 25;46(2):473-484.
Microorganisms

Isolation, Antimicrobial Susceptibility, and Genotypes of Three Pasteurellaeae Species Prevalent on Pig Farms in China Between 2021 and 2023. [Abstract]

2025 Apr 18;13(4):938. PMID: 40284774
Microorganisms

The Staphylococcus aureus ArlS Kinase Inhibitor Tilmicosin Has Potent Anti-Biofilm Activity in Both Static and Flow Conditions. [Abstract]

2024 Jan 25;12(2):256. PMID: 38399660
Vet Microbiol

Discovery of the tigecycline resistance gene cluster tmexCD3-toprJ1 in Pasteurella multocida strains isolated from pigs in China. [Abstract]

2024 May:292:110046. PMID: 38471428
bioRxiv

2026 Mar 25.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (103.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (103.40 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0340 mL

5.1699 mL

10.3399 mL

5 mM

0.2068 mL

1.0340 mL

2.0680 mL

10 mM

0.1034 mL

0.5170 mL

1.0340 mL

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (2.58 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.58 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: PBS

Solubility: 100 mg/mL (103.40 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (295 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ziv G, et al. Tilmicosin antibacterial activity and pharmacokinetics in cows. J Vet Pharmacol Ther. 1995 Oct;18(5):340-5. [Content Brief]

[2]. Buret AG. Immuno-modulation and anti-inflammatory benefits of antibiotics: the example of tilmicosin. Can J Vet Res. 2010 Jan;74(1):1-10. [Content Brief]

[3]. Cao XY, et al. Tilmicosin and tylosin have anti-inflammatory properties via modulation of COX-2 and iNOS gene expression and production of cytokines in LPS-induced macrophages and monocytes. Int J Antimicrob Agents. 2006 May;27(5):431-8. [Content Brief]

[4]. Ibrahim AE, et al. Modulating Effects of Spirulina platensis against Tilmicosin-Induced Cardiotoxicity in Mice. Cell J. 2015 Spring;17(1):137-44. [Content Brief]

[5]. Zhang N, et al. Pharmacokinetic and Pharmacodynamic integration of tilmicosin against Mycoplasma gallisepticum in the target infection site in chickens. Front Vet Sci. 2022 Sep 29;9:952599. [Content Brief]

[6]. Veenhuizen MF, et al. Analysis of reports of human exposure to Micotil 300 (tilmicosin injection). J Am Vet Med Assoc. 2006 Dec 1;229(11):1737-42. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	1.0340 mL	5.1699 mL	10.3399 mL	25.8497 mL
	5 mM	0.2068 mL	1.0340 mL	2.0680 mL	5.1699 mL
	10 mM	0.1034 mL	0.5170 mL	1.0340 mL	2.5850 mL
	15 mM	0.0689 mL	0.3447 mL	0.6893 mL	1.7233 mL
	20 mM	0.0517 mL	0.2585 mL	0.5170 mL	1.2925 mL
	25 mM	0.0414 mL	0.2068 mL	0.4136 mL	1.0340 mL
	30 mM	0.0345 mL	0.1723 mL	0.3447 mL	0.8617 mL
	40 mM	0.0258 mL	0.1292 mL	0.2585 mL	0.6462 mL
	50 mM	0.0207 mL	0.1034 mL	0.2068 mL	0.5170 mL
	60 mM	0.0172 mL	0.0862 mL	0.1723 mL	0.4308 mL
	80 mM	0.0129 mL	0.0646 mL	0.1292 mL	0.3231 mL
	100 mM	0.0103 mL	0.0517 mL	0.1034 mL	0.2585 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Tilmicosin phosphate

5 Cited Publications

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Tilmicosin phosphate

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Publications Citing Use of MedChemExpress (MCE) Tilmicosin phosphate

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle NO Synthase Isoform-spezifische Produkte anzeigen

Alle COX Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tilmicosin phosphate Related Classifications

Art. -Nr.: HY-B0905A