Tildipirosin

Veterinary antibiotic CAS# 328898-40-4

Tildipirosin

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Chemical structure

Tildipirosin

3D structure

Chemical Properties of Tildipirosin

Cas No. 328898-40-4 SDF Download SDF
PubChem ID 24860548 Appearance Powder
Formula C41H71N3O8 M.Wt 734.02
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (136.24 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (4R,5S,6S,7R,9R,11E,13E,15R,16R)-6-[(2R,3R,4S,5S,6R)-4-(dimethylamino)-3,5-dihydroxy-6-methyloxan-2-yl]oxy-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-piperidin-1-ylethyl)-15-(piperidin-1-ylmethyl)-1-oxacyclohexadeca-11,13-diene-2,10-dione
SMILES CCC1C(C=C(C=CC(=O)C(CC(C(C(C(CC(=O)O1)O)C)OC2C(C(C(C(O2)C)O)N(C)C)O)CCN3CCCCC3)C)C)CN4CCCCC4
Standard InChIKey HNDXPZPJZGTJLJ-UEJFNEDBSA-N
Standard InChI InChI=1S/C41H71N3O8/c1-8-35-32(26-44-20-13-10-14-21-44)23-27(2)15-16-33(45)28(3)24-31(17-22-43-18-11-9-12-19-43)40(29(4)34(46)25-36(47)51-35)52-41-39(49)37(42(6)7)38(48)30(5)50-41/h15-16,23,28-32,34-35,37-41,46,48-49H,8-14,17-22,24-26H2,1-7H3/b16-15+,27-23+/t28-,29+,30-,31+,32-,34-,35-,37+,38-,39-,40-,41+/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Tildipirosin

DescriptionTildipirosin, a long-acting macrolide, has antibiotic activity.In Vitro:Tildipirosin exhibits the inhibitory effect on C. coli species, and 23 of 31 (74%) isolates have MICs of 8 or 16 μg/mL while 8 of 31 (26%) have MIC >256 μg/mL. MICs against C. jejuni are 8-64 μg/mL. Tildipirosin against S. enterica and E. coli are 2-8 μg/mL[1]. Tildipirosin inhibits the treponeme isolates form from CODD lesions from 19 sheep, with MIC90 of 0.0469 mg/L[3]. The P. multocida B130 clones show the MIC of 0.25 mg/L for tildipirosin. The 10 P. multocida isolates that carry only erm(42) exhibit MIC of 16-32 mg/L for tildipirosin. The single M. haemolytica that harbours only erm(42) shows MIC of 32 mg/L for tildipirosin[4].In Vivo:The mean percentage of lung consolidation for tildipirosin (4 mg/kg, s.c.)-treated calves is significantly lower than those for tulathromycin-treated and control calves. Metaphylactic administration of tildipirosin to calves 5 days prior to H somni challenge prevents subsequent culture of the pathogen from bronchial secretions and is more effective in minimizing clinical disease and lung lesions than is metaphylactic administration of tulathromycin[2].

References:
[1]. Rose M, et al. A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs. J Vet Pharmacol Ther. 2016 Jun;39(3):277-86. [2]. Confer AW, et al. Clinical disease and lung lesions in calves experimentally inoculated with Histophilus somni five days after metaphylactic administration of tildipirosin or tulathromycin. Am J Vet Res. 2016 Apr;77(4):358-66. [3]. Angell JW, et al. In vitro susceptibility of contagious ovine digital dermatitis associated Treponema spp. isolates to antimicrobial agents in the UK. Vet Dermatol. 2015 Dec;26(6):484-7, e114-5. [4]. Michael GB, et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. J Antimicrob Chemother. 2012 Jun;67(6):1555-7.

Protocol

Animal Administration [2]
On day 0, each pen of 4 calves is randomly assigned by means of drawing numbers from a hat to receive 1 of 3 treatments; thus, each treatment group consists of 8 calves. Calves in group 1 receive tildipirosinb (4 mg/kg, SC), calves in group 2 receive tulathromycinc (2.5 mg/kg, SC), and calves in group 3 receive saline (0.9% NaCl) solution (1 mL/45 kg, SC; control). The volume of saline solution administered to the calves in group 3 approximates the volume of the assigned antimicrobial administered to the calves of groups 1 and 2. On day 5, all calves are experimentally inoculated (challenged) with 10 mL of PBS solution supplemented with 5% bovine fetal serum containing 1.6×109 CFUs of H somni/mL instilled via a flexible bronchoalveolar lavage tube (length, 3 m; external diameter, 11 mm; internal diameter, 3 mm) that is passed through the nasal passage and nasopharynx to the level of the tracheal bifurcation. Proper placement of the tube at the tracheal bifurcation is verified on the basis of qualitative observations that includ an elicited cough, absence of evidence of esophageal or ruminal placement as determined by smell and lack of tension and failure to observe the tube within the esophagus during placement, the presence of resistance at the carina, and the passage of the tube to a predetermined mark that approximates the distance from the nares to the carina. Following experimental inoculation, the tube is flushed with 60 mL of saline solution and 120 mL of air before it is removed from the calf. On day 8, all calves are weighed, sedated with xylazined (0.25 mg/kg), and transported in a trailer in groups of 4 to 6 calves. Immediately after euthanasia, a necropsy is performed on each calf.

References:
[1]. Rose M, et al. A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs. J Vet Pharmacol Ther. 2016 Jun;39(3):277-86. [2]. Confer AW, et al. Clinical disease and lung lesions in calves experimentally inoculated with Histophilus somni five days after metaphylactic administration of tildipirosin or tulathromycin. Am J Vet Res. 2016 Apr;77(4):358-66. [3]. Angell JW, et al. In vitro susceptibility of contagious ovine digital dermatitis associated Treponema spp. isolates to antimicrobial agents in the UK. Vet Dermatol. 2015 Dec;26(6):484-7, e114-5. [4]. Michael GB, et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. J Antimicrob Chemother. 2012 Jun;67(6):1555-7.

Tildipirosin Dilution Calculator

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Tildipirosin Molarity Calculator

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Preparing Stock Solutions of Tildipirosin

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.3624 mL 6.8118 mL 13.6236 mL 27.2472 mL 34.059 mL
5 mM 0.2725 mL 1.3624 mL 2.7247 mL 5.4494 mL 6.8118 mL
10 mM 0.1362 mL 0.6812 mL 1.3624 mL 2.7247 mL 3.4059 mL
50 mM 0.0272 mL 0.1362 mL 0.2725 mL 0.5449 mL 0.6812 mL
100 mM 0.0136 mL 0.0681 mL 0.1362 mL 0.2725 mL 0.3406 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Tildipirosin

Tildipirosin(Zuprevo) is a novel 16-membered macrolide for treatment, control, and prevention of bovine respiratory disease; inhibits protein synthesis on the ribosome (IC50= 0.23 ± 0.01 μM).

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References on Tildipirosin

Pharmacokinetics of tildipirosin in pig tonsils.[Pubmed:26935349]

J Vet Pharmacol Ther. 2016 Apr;39(2):199-201.

The penetration of antimicrobials in pig tonsils is hardly known. The objective of the study was to quantify the Tildipirosin (TD) penetration in tonsils. Animals were randomly divided into six groups (control, T1, T2 (1), T2(5), T2(10), and T2(15)) of eight animals. T1 and T2 groups received a dose of 2 and 4 mg of TD/kg bw in one shot (Zuprevo(R) MSD Animal Health), respectively, and the control group received 2 mL of saline solution. The animals were sacrificed by intravenous administration of pentobarbital sodium 24 h after finishing the treatment for the control, T1, and T2(1) groups, whereas animals of T2(5), T2(10), and T2(15) groups were sacrificed at 5, 10, and 15 days, post-treatment, respectively. Tonsils and blood samples were taken at necropsy to obtain plasma, and the Tildipirosin concentration was determined by high-performance liquid chromatography with tandem mass spectrometry detection. The concentration in plasma was always significantly lower than in tonsil. Average TD tonsil concentrations increased significantly in a dose-dependent manner, and the tonsil TD vs. plasma TD concentration ratio was approximately 75 for the doses of 2 and 4 mg of TD/kg bw at 24 h post-treatment. Moreover, the maximum concentration of Tildipirosin in tonsil was observed at 1 day postadministration, and this concentration decreased gradually from this day until 15 days postadministration for the dose of 4 mg of TD/kg bw. Finally, the ratio AUCtonsil/AUCplasma was 97.9, and the T1/2 (h) was clearly higher in tonsil than in plasma.

Clinical disease and lung lesions in calves experimentally inoculated with Histophilus somni five days after metaphylactic administration of tildipirosin or tulathromycin.[Pubmed:27027834]

Am J Vet Res. 2016 Apr;77(4):358-66.

OBJECTIVE: To compare clinical disease and lung lesions in calves experimentally inoculated with Histophilus somni 5 days after metaphylactic administration of Tildipirosin or tulathromycin. ANIMALS Twenty-four 3-month-old Holstein and Holstein-crossbreed steers. PROCEDURES: Calves were randomly allocated to 3 groups of 8 calves. On day 0, calves in group 1 received Tildipirosin (4 mg/kg, SC), calves in group 2 received tulathromycin (2.5 mg/kg, SC), and calves in group 3 received isotonic saline (0.9% NaCl) solution (1 mL/45 kg, SC; control). On day 5, calves were inoculated with 10 mL of a solution containing H somni strain 7735 (1.6 x 10(9) CFUs/mL, intrabronchially; challenge). Calves were clinically evaluated on days 5 through 8 and euthanized on day 8. The lungs were grossly evaluated for evidence of pneumonia, and bronchial secretion samples underwent bacteriologic culture. RESULTS: The mean clinical score for each group was significantly increased 12 hours after challenge, compared with that immediately before challenge, and was significantly lower for Tildipirosin-treated calves on days 6, 7, and 8, compared with those for tulathromycin-treated and control calves. The mean percentage of lung consolidation for Tildipirosin-treated calves was significantly lower than those for tulathromycin-treated and control calves. Histophilus somni was isolated from the bronchial secretions of some tulathromycin-treated and control calves but was not isolated from Tildipirosin-treated calves. CONCLUSIONS AND CLINICAL RELEVANCE: Results indicated that metaphylactic administration of Tildipirosin to calves 5 days prior to H somni challenge prevented subsequent culture of the pathogen from bronchial secretions and was more effective in minimizing clinical disease and lung lesions than was metaphylactic administration of tulathromycin.

Efficacy of tildipirosin metaphylaxis for the prevention of respiratory disease, otitis and mortality in pre-weaned Holstein calves.[Pubmed:28093111]

Vet J. 2017 Jan;219:44-48.

The aim of this study was to evaluate the efficacy of two metaphylactic approaches (long acting antibiotic injected once at 10 days of life or twice at 10 and 35 days of life) on the prevention of bovine respiratory disease (BRD), otitis and mortality in high-risk group-housed pre-weaned Holstein heifer calves. The antibiotic of choice for the metaphylactic approach was a long acting macrolide (Tildipirosin) administered subcutaneously at the base of the neck at a dose of 1 mL per 45 kg body weight. A clinical trial was carried out on one dairy farm with random allocation of newborn calves to one of three treatments: (1) control (CTR); (2) one injection at 10 days of life (M1); and (3) two injections at 10 and 35 days of life (M2). Study heifers (n = 795) were reared in group pens of 25 calves per pen and fed unrestricted acidified non-saleable milk from day 1 to day 65 of life. Cox proportional hazard and general linear mixed models were used to evaluate the effect of treatment on mortality, BRD and otitis, and average daily weight gain. The birth weights, proportions of calves with inadequate transfer of passive immunity, proportions of calves born from primiparous dams and proportions of calves born from assisted parturitions were not different among CTR, M1 and M2 treatments. A significantly lower hazard of being affected with BRD and/or otitis (but not for BRD or otitis alone) was observed for M1 (hazard ratio, HR = 0.70, P = 0.009) and M2 (HR = 0.72, P = 0.01) when compared to the CTR group. Metaphylactic treatments had no effect on mortality, otitis and average daily weight gain during the pre-weaning period.

A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs.[Pubmed:26538405]

J Vet Pharmacol Ther. 2016 Jun;39(3):277-86.

Tildipirosin (TIP) is a novel 16-membered-ring macrolide authorized for the treatment of bovine and swine respiratory disease. The pH dependency of macrolide antimicrobial activity is well known. Considering that the pH in the colon contents of growing beef cattle and pigs is usually below pH 7.0, the minimum inhibitory concentrations (MIC) of TIP against foodborne bacterial pathogens such as Campylobacter (C.) coli, C. jejuni and Salmonella enterica and commensal species including Enterococcus (E.) faecalis, E. faecium and Escherichia coli were determined under standard (pH 7.3 +/- 1) or neutral as well as slightly acidic conditions. A decrease in pH from 7.3 to 6.7 resulted in an increase in MICs of TIP. Except for the MICs > 256 mug/mL observed in the resistant subpopulation of the C. coli and the Enterococcus species, the MIC ranges increased from 2-8 mug/mL to 64-> 256 mug/mL for Salmonella enterica and E. coli, from 8-16 mug/mL to 32-128 mug/mL for the two Campylobacter species, and from 4-32 mug/mL to 128-> 256 mug/mL for both Enterococcus species. To estimate the antimicrobial activity of TIP in the colon contents of livestock during recommended usage of the parenterally administered TIP (Zuprevo((R)) ), and to compare this with the increased MICs at the slightly acidic colonic pH, we developed and validated a microbiological assay for TIP and used this to test incurred faecal samples collected from cattle and pigs. Microbiological activity of luminal TIP was determined in aqueous supernatants from diluted faeces, using standard curves produced from TIP-spiked faecal supernatants. The limit of quantification (LOQ) for TIP was 1 mug/mL (ppm). In a cattle study (n = 14), 3 of 28 faecal samples collected 24 and 48 h post-treatment were found to contain TIP above the LOQ (concentrations of 1.3-1.8 ppm). In another cattle study (n = 12) with faecal samples collected at 8, 24 and 48 h post-treatment, TIP concentrations were above the LOQ in 4 of the 8 h samples (1.2-2.6 ppm) and one of the 24-h samples (1.3 ppm). In a pig study (n = 12) with faecal samples collected 24, 48 and 72 h post-treatment, only one sample contained TIP above the LOQ (concentration 1.5 ppm). In another pig study (n = 12), with samples collected at 8, 24 48 and 96 h post-treatment, TIP concentrations were above the LOQ in one 8-h sample (1.1 ppm) and two 24-h samples (2.3 and 2.5 ppm). None of the 48-h and 96-h samples from these 4 studies contained measurable TIP concentrations. Thus, in cattle and pigs, only a small fraction of faecal samples collected up to 24 h postdosing contained measurable microbiologically active TIP, with its maximum limited to 2.6 mug/mL. This is several log2 dilution steps below the MICs of TIP against foodborne pathogens and commensals collected under acidic conditions comparable with those in the colonic contents and may explain a lack of intestinal dysbacteriosis with parenteral Tildipirosin in livestock.

Description

Tildipirosin, a long-acting macrolide, has antibiotic activity.

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