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Tulathromycin A

Catalog No.
A3896
Triamilide antimicrobial
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$143.00
In stock
10mg
$137.00
In stock
50mg
$570.00
In stock

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Background

Tulathromycin A is a macrolide antibiotic [1].Antibiotics are a type of antimicrobial used in the treatment and prevention of bacterial infection.
Two highly pathogenic strains of M. bovis were incubated into 145 calves. Four days later, calves with clinical BRD were treated subcutaneously with tulathromycin or saline (2.5 mg/kg). BRD-related withdrawals, peak rectal temperatures, and lung lesion scores were significantly lower for tulathromycin-treated calves [2]. In the treatment of cattle at high risk of developing bovine respiratory disease, the cure rate treated with tulathromycin (78%) and tilmicosin (65%) was significantly higher than that treated with saline (23.8%). The cure rate treated with tulathromycin (78.4%) was also significantly higher than tilmicosin (64.9%) [3].
The lowest tulathromycin concentrations inhibiting the 90% growth of isolates (MIC90) were 2 μg/ml for Mannheimia (Pasteurella) haemolytica, 1 μg/ml for Pasteurella multocida (bovine), and 2 μg/ml for Pasteurella multocida (porcine) and ranged from 0.5-4 μg/ml for Histophilus somni and from 4-16 μg/ml for Actinobacillus pleuropneumoniae [1]. Tulathromycin has been approved for use in the treatment and prevention of swine and bovine respiratory disease [1].
References:
[1]. Godinho KS, et al. Minimum inhibitory concentrations of tulathromycin against respiratory bacterial pathogens isolated from clinical cases in European cattle and swine and variability arising from changes in in vitro methodology.Vet Ther, 2005, 6(2): 113-121.
[2]. Godinho KS, et al. Efficacy of tulathromycin in the treatment of bovine respiratory disease associated with induced Mycoplasma bovis infections in young dairy calves.Vet Ther, 2005, 6(2): 96-112.
[3]. Kilgore WR, Spensley MS, Sun F, et al. Therapeutic efficacy of tulathromycin, a novel triamilide antimicrobial, against bovine respiratory disease in feeder calves.Vet Ther, 2005, 6(2): 143-153.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt806.08
Cas No.217500-96-4
FormulaC41H79N3O12
SynonymsTulathromycin;Draxxin;CP 472295
Solubility≥24.1 mg/mL in DMSO, ≥96.8 mg/mL in EtOH,insoluble in H2O
Chemical Name11-((4-(dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-2-ethyl-3,4,10-trihydroxy-13-((5-hydroxy-4-methoxy-4,6-dimethyl-5-((propylamino)methyl)tetrahydro-2H-pyran-2-yl)oxy)-3,5,8,10,12,14-hexamethyl-1-oxa-6-azacyclopentadecan-15-one
SDFDownload SDF
Canonical SMILESCCCNCC1(O)C(C)OC(OC2C(C)C(OC3C(O)C(N(C)C)CC(C)O3)C(C)(O)CC(C)CNC(C)C(O)C(C)(O)C(CC)OC(C2C)=O)CC1(OC)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

E.coli, Mannheimia haemolytica, Pasteurella multocida

Preparation method

The solubility of this compound in DMSO is ≥24.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.5μg/ml-16μg/ml

Applications

Tulathromycin A is a macrolide antibiotic that inhibits bacterial protein synthesis by acting on the 50S ribosomal subunit (IC50 = 0.26 µM), preventing the formation of new polypeptide chains.

Animal experiment [1]:

Animal models

Cattle and swine

Dosage form

2.5 mg/kg(i.m.)

Application

In cattle and swine, tulathromycin is characterized by a fast absorption rate for subcutaneous (s.c.) and intramuscular (i.m.) administration and high systemic availability. In contrast, oral tulathromycin with a compound preparation had a lower systemic availability (~ 50%). In plasma, tulathromycin has a long terminal half-life, which ranges from ~ 2 to ~ 5 days except that the mouse terminal half-life is less than 20 hours. The longest terminal half-life in plasma can be seen in foals (~ 140 hours).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Andersen NM, Poehlsgaard J, Warrass R, Douthwaite S. Inhibition of protein synthesis on the ribosome by tildipirosin compared with other veterinary macrolides. Antimicrob Agents Chemother. 2012 Nov;56(11):6033-6. doi: 10.1128/AAC.01250-12. Epub 2012 Aug 27. PMID: 22926570; PMCID: PMC3486562.

[2]. Villarino N, Brown SA, Martín-Jiménez T. Understanding the pharmacokinetics of tulathromycin: a pulmonary perspective. J Vet Pharmacol Ther. 2014 Jun;37(3):211-21. doi: 10.1111/jvp.12080. Epub 2013 Sep 30. PMID: 24117832.

Quality Control

Quality Control & MSDS

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Chemical structure

Tulathromycin A