| 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 therapy has been associated with mild and transient serum aminotransferase elevations that were generally self-limited and only slightly more common with ticarcillin than with comparative antibiotics. Much more commonly reported were instances of anicteric hepatic injury from carbenicillin, a similar carboxypenicillin with extend coverage against Pseudomonas. Persons receiving high doses of intravenous carbenicillin not uncommonly (15% to 30%) developed serum aminotransferase elevations without jaundice, which promptly fell to normal with discontinuation or switching to another antibiotic. Recurrence is common with retreatment using carbenicillin, but not with ticarcillin. A similar phenomenon occurs with intravenous oxacillin. Rare instances of idiosyncratic, clinically apparent cholestatic liver injury have been reported in persons receiving ticarcillin in combination with clavulanate, some of which resemble the rare idiosyncratic reactions that can occur with many penicillins and which resemble the cholestatic liver injury that occurs after amoxicillin/clavulanate. Likelihood score: D (possible rare cause of clinically apparent liver injury). Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation Limited information indicates that ticarcillin produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with penicillins, but these effects have not been adequately evaluated. Ticarcillin is acceptable in nursing mothers. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding 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 having a 6beta-[(2R)-2-carboxy-2-thiophen-3-ylacetyl]amino side-group. It has a role as an antibacterial drug. It is a penicillin and a penicillin allergen. It is a conjugate acid of a ticarcillin(2-).
An antibiotic derived from penicillin similar to carbenicillin in action. Ticarcillin is a Penicillin-class Antibacterial. Ticarcillin is an extended-spectrum carboxypenicillin antibiotic and is used to treat moderate-to-severe infections due to susceptible organisms. Ticarcillin has been linked with idiosyncratic liver injury, but only rarely and as isolated case reports. Ticarcillin has been reported in Brassica napus and Apis cerana with data available. Ticarcillin is a broad-spectrum, semi-synthetic penicillin antibiotic with bactericidal activity. Similar to carbenicillin in action, ticarcillin inactivates the penicillin-sensitive transpeptidase C-terminal domain by opening the lactam ring. This inactivation prevents the cross-linkage of peptidoglycan strands, thereby inhibiting the third and last stage of bacterial cell wall synthesis. This leads to incomplete bacterial cell wall synthesis and eventually causes cell lysis. An antibiotic derived from penicillin similar to CARBENICILLIN in action. Drug Indication For the treatment of bacterial infections. Mechanism of Action Ticarcillin's principal mechanism of action revolves around its capacity to prevent the cross-linking of peptidoglycan during bacterial cell wall synthesis. Consequently, when the offending bacteria attempt to undergo cell division, cell death occurs. Pharmacodynamics Ticarcillin is a semisynthetic antibiotic with a broad spectrum of bactericidal activity against many gram-positive and gram-negative aerobic and anaerobic bacteria. Ticarcillin is, however, susceptible to degradation by ß-lactamases, and therefore, the spectrum of activity does not normally include organisms which 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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