| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
CYP2 CYP3
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|---|---|
| ln Vitro |
Ticlopidine displays activity at apparent Ki,app values of 14 µM against human CD39[1]. Ticlopidine has a Ki value of 127±12 µM, which inhibits recombinant human CD39 expressed in COS-7-cells[1]. Ticlopidine (30 and 150 µM) has an impact on growth rate in the first few days of culture, but its effects diminish in the days that follow[4].
|
| ln Vivo |
Ticlopidine can effectively prevent losartan metabolism in the intestine and/or liver when given orally in combination with Losartan at a dose of 10 mg/kg. This is indicated by the considerable rise in the AUC (by 65.0%) observed by this combination[3].
|
| Cell Assay |
Cell Proliferation Assay[4]
Cell Types: Human endothelial cells Tested Concentrations: 30 and 150 µM Incubation Duration: 2, 6; 10 days Experimental Results: Treated cells grow slower if compared with controls and this effect correlates with the concentration of Ticlopidine in the culture medium. |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats ( 7-8 weeks old, weighing 270-300 g)[3]
Doses: 4 or 10 mg/kg Route of Administration: Orally administered 30 min before oral administration of losartan. Experimental Results: The AUC and Cmax of Losartan after oral administration with Losartan and 10 mg/kg Ticlopidine were Dramatically greater (by 65.0% and 49.4%, respectively) than those of control rats. |
| References |
[1]. Laura Schäkel, et al. 2-Substituted thienotetrahydropyridine derivatives: Allosteric ectonucleotidase inhibitors. Arch Pharm (Weinheim). 2021 Dec;354(12):e2100300.
[2]. I.KRASLOVA1, et al. Ticlopidine-Induced Cholestatic Inflammatory Hepatitis: New Insights into Pathogenetic Mechanisms of Drug-Related Hepatotoxicity. [3]. Si-hyung Yang, et al. Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats. Acta Pharmacol Sin. 2011 Jul;32(7):967-72. [4]. F Piovella, et al. The effect of Ticlopidine on human endothelial cells in culture. Thromb Res. 1984 Feb 1;33(3):323-32. |
| Molecular Formula |
C14H14CLNS
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|---|---|
| Molecular Weight |
263.79
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| CAS # |
55142-85-3
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| Related CAS # |
Ticlopidine hydrochloride;53885-35-1;Ticlopidine-d4;1246817-49-1
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| SMILES |
ClC1=C([H])C([H])=C([H])C([H])=C1C([H])([H])N1C([H])([H])C2C([H])=C([H])SC=2C([H])([H])C1([H])[H]
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| Solubility (In Vitro) |
DMSO: ≥ 100 mg/mL (379.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.48 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7909 mL | 18.9545 mL | 37.9089 mL | |
| 5 mM | 0.7582 mL | 3.7909 mL | 7.5818 mL | |
| 10 mM | 0.3791 mL | 1.8954 mL | 3.7909 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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