| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Tildipirosin targets the bacterial 50S ribosomal subunit, inhibiting protein synthesis. Like other macrolides, it binds to the 23S rRNA of the 50S ribosomal subunit, blocking the exit tunnel for nascent peptides and preventing translation elongation. This results in inhibition of bacterial protein synthesis and growth. Its spectrum of activity is wider than that of dibasic analogs such as tilmicosin.
|
|---|---|
| ln Vitro |
Tildipirosin inhibited the growth of E. Coli, of which 8 of the 31 isolates (26%) had a MIC >256 μg/mL and 23 of the 31 isolates (74%) had a MIC of 8 or 16 μg/mL. ..For Campylobacter jejuni, the MIC ranges from 8 to 64 μg/mL. Tedikicin has a concentration of 2–8 μg/mL against Escherichia coli and Salmonella enterica[1]. Treponemal isolates from 19 sheep with CODD lesions were suppressed by tildipirosin, with a MIC90 of 0.0469 mg/L [3]. Tediloxin MIC was 0.25 mg/L for the Pasteurella multocida B130 clone. Ten isolates of Pseudomonas multocida that solely have erm(42) had MICs for tedirocin ranging from 16 to 32 mg/L. Just one M. The TEDIloxin MIC of 32 mg/L was observed in haemolyticus bearing just erm(42) [4].
In vitro, tildipirosin is a potent antimicrobial agent. It exhibits activity against Gram-negative bacteria, including Mycoplasma spp. It shows good protection against Pasteurella. Its antibacterial activity is confirmed in standard antimicrobial susceptibility tests, with minimum inhibitory concentrations (MICs) varying depending on the organism. |
| ln Vivo |
In comparison to calves treated with tulathromycin and control, the mean percentage of lung consolidation in calves treated with tediloxin (4 mg/kg, subcutaneously) was considerably lower. In comparison to the dry prophylactic administration of telamycin Clinical illnesses and lung lesions, the dry prophylactic injection of tediloxin to calves five days prior to a sleep hemophilia challenge prevented subsequent culture of the pathogen from bronchial secretions[2].
In vivo, tildipirosin is used in veterinary medicine to treat respiratory infections in cattle and swine. It is a long-acting macrolide antibiotic. It is marketed under the brand name Zuprevo. It is effective against pathogens such as Mannheimia haemolytica, Pasteurella multocida, and Actinobacillus pleuropneumoniae. It has a prolonged duration of action. |
| Enzyme Assay |
Cell-free assays for tildipirosin are not typical because its antibacterial activity is assessed using microbiological methods. However, its binding to the 50S ribosomal subunit can be studied using ribosome binding assays. Its inhibition of protein synthesis can be assessed using cell-free translation assays with bacterial lysates. Its purity is confirmed by HPLC.
|
| Cell Assay |
Cellular assays for tildipirosin are performed using standard microbiological susceptibility testing methods. The minimum inhibitory concentration (MIC) is determined using broth dilution or agar dilution methods according to CLSI guidelines. Susceptibility testing is performed using a range of bacterial strains, including respiratory pathogens.
|
| Animal Protocol |
In vivo animal experiments for tildipirosin are conducted in cattle and swine models of respiratory disease. Animals are infected with bacterial pathogens and treated with tildipirosin via injection. Clinical signs, bacterial clearance, and survival are assessed. Pharmacokinetic studies are also performed to determine drug concentrations in plasma and tissues.
|
| ADME/Pharmacokinetics |
Tildipirosin has a molecular weight of 734.97 g/mol and a molecular formula of C41H71N3O8. It is a 16-membered ring macrolide. It is a white to off-white powder. It is soluble in organic solvents and should be stored under recommended conditions. Its pharmacokinetic properties include a long half-life and high tissue penetration.
|
| Toxicity/Toxicokinetics |
The toxicological profile of tildipirosin is typical of macrolide antibiotics. It is generally well-tolerated in animals. Common side effects include injection site reactions and gastrointestinal disturbances. It is contraindicated in animals with known hypersensitivity to macrolides. Its safety has been established through veterinary use.
|
| 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]. 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. [3]. 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. [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 |
| Additional Infomation |
Tildipirosin is a veterinary antibiotic.
Indications 40 mg/ml injection, for swine: Used for the treatment and prevention of swine respiratory disease (SRD) caused by Actinobacillus pleuropneumoniae, Pasteurella multocida, Bordezoella bronchiseptica, and Haemophilus parasuis, all sensitive to tildemirocin. Before administering prophylactic treatment, the presence of the disease in the herd should be confirmed. 180 mg/ml injection, for bovine respiratory disease (BRD) caused by Mannella hemolyticus, Pasteurella multocida, and Haemophilus, all sensitive to tildemirocin. Before administering prophylactic treatment, the presence of the disease in the herd should be confirmed. Tildipirosin is a veterinary macrolide antibiotic used to treat respiratory diseases in cattle and swine. It is a derivative of tylosin and a 16-membered ring macrolide. It is marketed under the brand name Zuprevo. It inhibits bacterial protein synthesis and has a broad spectrum of activity. It is not approved for human use. |
| Molecular Formula |
C41H71N3O8
|
|---|---|
| Molecular Weight |
734.03
|
| Exact Mass |
733.524
|
| Elemental Analysis |
C, 67.09; H, 9.75; N, 5.72; O, 17.44
|
| CAS # |
328898-40-4
|
| PubChem CID |
24860548
|
| Appearance |
Solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
846.8±65.0 °C at 760 mmHg
|
| Flash Point |
465.9±34.3 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.557
|
| LogP |
4.7
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
52
|
| Complexity |
1170
|
| Defined Atom Stereocenter Count |
12
|
| SMILES |
O=C(/C=C/C(C)=C/[C@H](CN1CCCCC1)[C@@H](CC)O2)[C@H](C)C[C@H](CCN3CCCCC3)[C@H](OC4[C@@H](O)[C@@H](N(C)C)[C@H](O)[C@H](C)O4)[C@@H](C)[C@H](O)CC2=O
|
| InChi Key |
HNDXPZPJZGTJLJ-UEJFNEDBSA-N
|
| InChi Code |
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
|
| 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
|
| Synonyms |
Zuprevo; Tildipirosin; TIP
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~136.24 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3623 mL | 6.8117 mL | 13.6234 mL | |
| 5 mM | 0.2725 mL | 1.3623 mL | 2.7247 mL | |
| 10 mM | 0.1362 mL | 0.6812 mL | 1.3623 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
