product name Ticlopidine HCl
Description: Ticlopidine HCl is a potent P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM. Ticlopidine is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor. Initial research showed that Ticlopidine was useful for preventing strokes and coronary stent occlusions. However, due to its serious side effects of neutropenia and thrombotic thrombocytopenic purpura, Ticlopidine was primarily used in patients in whom aspirin was not tolerated, or in whom dual antiplatelet therapy was desirable.
References: Clin Pharmacol Ther. 1975 Oct;18(4):485-90; Thromb Haemost. 1979 Apr 23;41(2):436-49.
300.25
Formula
C14H14ClNS.HCl
CAS No.
53885-35-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 1 mg/mL (3.3 mM)
Water: 4 mg/mL (13.3 mM)
Ethanol: 1 mg/mL (3.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Ticlopidine HCl is an antiplatelet drug in the thienopyridine family. Ticlopidine HCl inhibits platelet aggregation by altering the function of platelet membranes by blocking ADP receptors. This prevents the conformational change of glycoprotein IIb/IIIa which allows platelet binding to fibrinogen. Ticlopidine HCl inhibits platelet aggregation and prostaglandin synthesis from endogenous substrate through activating basal and PGE1-stimulated activity of the cyclase, preventing PGE2-induced depression of the cyclase activity and thus increasing platelet c-AMP level. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Ticlopidine HCl inhibits platelet aggregation with IC50 of ~2 μM in men. Ticlopidine HCl, when orally administered to rats, results in activation of basal and prostaglandin E1 (PGE1)-stimulated adenylate cylase activity through increase in affinity of the cyclase in platelet membrane to PGE1, although it failed to affect adenosine- or sodium fluoride-stimulated activity of the enzyme. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Pharmacol Ther. 1975 Oct;18(4):485-90; Thromb Haemost. 1979 Apr 23;41(2):436-49. |
