Ticlopidine
Based on 3 publication(s) in Google Scholar
Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
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- 純度: 99.74%
- CAS 番号: 55142-85-3
- 分子式: C14H14ClNS
- 分子量:263.79
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Ticlopidine
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生物活性
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CYP2 |
CYP3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
0.36 μM
Compound: Ticlid
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Inhibition of ADP-induced platelet aggregation in New Zealand White rabbit
Inhibition of ADP-induced platelet aggregation in New Zealand White rabbit
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[PMID: 38704941] |
| Platelet | IC50 |
3.18 μM
Compound: Ticlopidine
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Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation treated for 5 mins before ADP challenge measured for 6 mins by microplate reader
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of ADP-induced platelet aggregation treated for 5 mins before ADP challenge measured for 6 mins by microplate reader
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[PMID: 22137848] |
| Platelet | IC50 |
3.72 μM
Compound: Ticlopidine
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Antiplatelet activity in New Zealand rabbit platelet-rich plasma assessed as inhibition of ADP-induced aggregation treated for 5 mins prior to ADP-challenge measured after 1 to 6 mins by spectrophotometric analysis
Antiplatelet activity in New Zealand rabbit platelet-rich plasma assessed as inhibition of ADP-induced aggregation treated for 5 mins prior to ADP-challenge measured after 1 to 6 mins by spectrophotometric analysis
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[PMID: 24565904] |
| Sf21 | IC50 |
49 μM
Compound: Ticlopidine
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
74 μM
Compound: Ticlopidine
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
Ticlopidine exhibits activity against human CD39 with apparent Ki,app values of 14 µM[1].
Ticlopidine inhibits recombinant human CD39 expressed in COS-7-cells with the Ki value of 127±12 µM[1].
Growth rate is affected during the first days of culture, Ticlopidine (30 and 150 µM) reducing its effect in the following days[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human endothelial cells
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Concentration:30 and 150 µM
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Incubation Time:2, 6; 10 days
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Result:Treated cells grow slower if compared with controls and this effect correlates with the concentration of Ticlopidine in the culture medium.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (7-8 weeks old, weighing 270-300 g)[3]
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Dosage:4 or 10 mg/kg
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Administration:Orally administered 30 min before oral administration of losartan.
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Result:The AUC and Cmax of Losartan after oral administration with Losartan and 10 mg/kg Ticlopidine were significantly greater (by 65.0% and 49.4%, respectively) than those of control rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 55142-85-3
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性状 Solid
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分子量 263.79
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分子式 C14H14ClNS
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Color Off-white to light yellow
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SMILES
ClC1=CC=CC=C1CN2CCC3=C(C=CS3)C2
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別名
PCR 5332
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
A Computational Integration Strategy Driven by Chemical Similarity Uncovers Comprehensive Metabolic Profiles of Small Bioactive Peptides via UHPLC-HRMS for Doping Control. [Abstract]2025 Nov 18;97(45):25158-25167. PMID: 41202118 -
Biochem Biophys Res Commun
2024 Jul 23:733:150436. PMID: 39053102
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (379.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Laura Schäkel, et al. 2-Substituted thienotetrahydropyridine derivatives: Allosteric ectonucleotidase inhibitors. Arch Pharm (Weinheim). 2021 Dec;354(12):e2100300. [Content Brief]
[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. [Content Brief]
[4]. F Piovella, et al. The effect of Ticlopidine on human endothelial cells in culture. Thromb Res. 1984 Feb 1;33(3):323-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7909 mL | 18.9545 mL | 37.9089 mL | 94.7724 mL |
| 5 mM | 0.7582 mL | 3.7909 mL | 7.5818 mL | 18.9545 mL | |
| 10 mM | 0.3791 mL | 1.8954 mL | 3.7909 mL | 9.4772 mL | |
| 15 mM | 0.2527 mL | 1.2636 mL | 2.5273 mL | 6.3182 mL | |
| 20 mM | 0.1895 mL | 0.9477 mL | 1.8954 mL | 4.7386 mL | |
| 25 mM | 0.1516 mL | 0.7582 mL | 1.5164 mL | 3.7909 mL | |
| 30 mM | 0.1264 mL | 0.6318 mL | 1.2636 mL | 3.1591 mL | |
| 40 mM | 0.0948 mL | 0.4739 mL | 0.9477 mL | 2.3693 mL | |
| 50 mM | 0.0758 mL | 0.3791 mL | 0.7582 mL | 1.8954 mL | |
| 60 mM | 0.0632 mL | 0.3159 mL | 0.6318 mL | 1.5795 mL | |
| 80 mM | 0.0474 mL | 0.2369 mL | 0.4739 mL | 1.1847 mL | |
| 100 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.9477 mL |
Ticlopidine 関連分類
HY-100386 関連分類
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