| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Ticarcillin therapy (10 mg/L; 18 hours) demonstrated antibacterial action [1].
|
|---|---|
| ln Vivo |
A dose-dependent antibacterial action is shown when ticarcillin (subcutaneous injection; 50, 100, or 200 mg/kg; once) is administered [2]. Excellent pharmacokinetic evaluation was shown when ticarcillin (subcutaneous injection; 50, 100, or 200 mg/kg; once) was administered [2].
|
| Cell Assay |
Cell viability assay[2]
Cell Types: Ps. Pseudomonas aeruginosa Tested Concentrations: 10 mg/L Incubation Duration: 18 hrs (hours) Experimental Results: It shows that the MIC of ticarcillin against the strain is between 6.3-12.5 mg/L. |
| Animal Protocol |
Animal/Disease Models: Swiss-type male mice injected with Ps. Pseudomonas aeruginosa [2]
Doses: 50, 100, 200 mg/kg Route of Administration: subcutaneous injection; 50, 100, 200 mg/kg; Experimental Results:As the dose increases, the effect is Dramatically enhanced (0.001 < P < 0.0025). Animal/Disease Models: Swiss-type male mice injected with Ps. Pseudomonas aeruginosa[2] Doses: 50, 100, 200 mg/kg Route of Administration: subcutaneous injection; 50, 100, 200 mg/kg; primary Experimental Results: Dose (mg/kg) AUCa (mg/kg) Kelb (h-1) T1/2 (min) Ticarcillin 50 8.76 (0.72) 1.57 (0.18) 26 100 26.14 (0.60) 1.53 (0.11) 27 200 54.56 (2.90) 1.47 (0.12) 28 |
| ADME/Pharmacokinetics |
Biological Half-Life
1.1 hours |
| Toxicity/Toxicokinetics |
Hepatotoxicity
Intravenous ticarcillin treatment is associated with mild, transient elevations in serum transaminases, which usually resolve spontaneously, and the incidence in the ticarcillin group is only slightly higher than with other antibiotics in the same class. More commonly, non-jaundiced liver injury is caused by carbazin (a carboxypenicillin similar to ticarcillin with a broader antibacterial spectrum against Pseudomonas aeruginosa). A significant proportion (15% to 30%) of patients receiving high-dose intravenous carbazin experience elevated serum transaminases without jaundice; these levels rapidly return to normal upon discontinuation of the drug or switching to another antibiotic. Relapse of hepatotoxicity is more common with re-treatment with carbazin, but not with ticarcillin. Similar phenomena can occur with intravenous oxacillin. Rare, specific, clinically well-presented cases of cholestatic liver injury have been reported in patients receiving ticarcillin in combination with clavulanate potassium. Some of these cases resemble rare, specific reactions that can occur with many penicillin-type drugs, as well as cholestatic liver injury following amoxicillin/clavulanate potassium treatment. Probability Score: D (Possibly a rare cause of clinically significant liver injury). Use during Pregnancy and Lactation ◉ Overview of Use during Lactation Limited information suggests that ticarcillin concentrations in breast milk are low and are not expected to have adverse effects on breastfed infants. There have been reports of penicillin-type drugs occasionally disrupting the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been adequately assessed. Ticarcillin can be used in breastfeeding women. ◉ Effects on Breastfed Infants No relevant published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No relevant published information found as of the revision date. Protein Binding Rate 45% |
| References |
[1]. Cecile Formosa, et al. Nanoscale effects of antibiotics on P. aeruginosa. Nanomedicine. 2012 Jan;8(1):12-6.
[2]. G B van der Voet, et al. Comparison of the antibacterial activity of azlocillin and ticarcillin in vitro and in irradiated neutropenic mice. J Antimicrob Chemother. 1985 Nov;16(5):605-13. [3]. Oriel Spierer, et al. Comparative activity of antimicrobials against Pseudomonas aeruginosa, Achromobacter xylosoxidans and Stenotrophomonas maltophilia keratitis isolates. Br J Ophthalmol. 2018 May;102(5):708-712. |
| Additional Infomation |
Ticarcillin is a penicillin compound with a side chain containing 6β-[(2R)-2-carboxy-2-thiophene-3-ylacetyl]amino. It is an antibacterial drug. It is both a penicillin compound and a penicillin allergen. It is the conjugate acid of ticarcillin (2-). Ticarcillin is a penicillin-derived antibiotic with a mechanism of action similar to carbenicillin. Ticarcillin belongs to the penicillin class of antibacterial drugs. Ticarcillin is a broad-spectrum carboxylic acid antibiotic used to treat moderate to severe infections caused by susceptible bacteria. Ticarcillin has been associated with specific liver injury, but this is very rare, with only isolated case reports. There are reports of ticarcillin causing liver injury in Brassica napus and Apis cerana, and relevant data are available. Ticarcillin is a broad-spectrum semi-synthetic penicillin antibiotic with bactericidal activity. Its mechanism of action is similar to carbenicillin; ticarcillin inactivates the penicillin-sensitive C-terminal domain of transpeptidase by opening the lactam ring. This inactivation prevents the cross-linking of peptidoglycan chains, thereby inhibiting the third and final stage of bacterial cell wall synthesis. This leads to incomplete bacterial cell wall synthesis, ultimately resulting in cell lysis.
An antibiotic derived from penicillin, with a mechanism of action similar to carbenicillin. Indications For the treatment of bacterial infections. Mechanism of Action The main mechanism of action of ticarcillin is its ability to prevent the cross-linking of peptidoglycan during bacterial cell wall synthesis. Therefore, cell death occurs when pathogenic bacteria attempt to divide. Pharmacodynamics Ticarcillin is a semi-synthetic antibiotic with broad-spectrum bactericidal activity against a variety of Gram-positive and Gram-negative aerobic and anaerobic bacteria. However, ticarcillin is susceptible to degradation by β-lactamases; therefore, its antibacterial spectrum typically does not include microorganisms that produce these enzymes. |
| Molecular Weight |
428.39106
|
|---|---|
| Exact Mass |
384.044
|
| CAS # |
34787-01-4
|
| Related CAS # |
(2S,5R,6R)-Ticarcillin disodium;4697-14-7;Ticarcillin sodium;29457-07-6
|
| PubChem CID |
36921
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
768.3±60.0 °C at 760 mmHg
|
| Flash Point |
418.4±32.9 °C
|
| Vapour Pressure |
0.0±2.7 mmHg at 25°C
|
| Index of Refraction |
1.694
|
| LogP |
0.69
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
25
|
| Complexity |
640
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O=C([C@H]1C(C)(C)S[C@H]2N1C([C@H]2NC([C@H](C(O)=O)c1c[s]cc1)=O)=O)O
|
| InChi Key |
OHKOGUYZJXTSFX-KZFFXBSXSA-N
|
| InChi Code |
InChI=1S/C15H16N2O6S2/c1-15(2)9(14(22)23)17-11(19)8(12(17)25-15)16-10(18)7(13(20)21)6-3-4-24-5-6/h3-5,7-9,12H,1-2H3,(H,16,18)(H,20,21)(H,22,23)/t7-,8-,9+,12-/m1/s1
|
| Chemical Name |
(2S,5R,6R)-6-[[(2R)-2-carboxy-2-thiophen-3-ylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3343 mL | 11.6716 mL | 23.3432 mL | |
| 5 mM | 0.4669 mL | 2.3343 mL | 4.6686 mL | |
| 10 mM | 0.2334 mL | 1.1672 mL | 2.3343 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.
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