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MedChemExpress - Model Tilmicosin phosphate - 137330-13-3

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[1][2][3][4][5][6].

Tilmicosin phosphate

MCE China：Tilmicosin phosphate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0905A

CAS：137330-13-3

Synonyms：LY-177370 phosphate; EL-870 phosphate

Purity：98.0%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

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) 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

IC50 & Target：COX-2

References：

[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]

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