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编 号:F387575
分子式:C14H14ClNS
分子量:263.79
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

体内研究:
Oral administration of Losartan with 10 mg/kg Ticlopidine significantly increases the AUC (by 65.0%), suggesting that Ticlopidine can effectively inhibit the metabolism of losartan in the intestine and/or liver.Animal Model:Male Sprague-Dawley rats (7-8 weeks old, weighing 270-300 g)
Dosage:4 or 10 mg/kg
Administration:Orally administered 30 min before oral administration of losartan.
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.

体外研究:
Ticlopidine exhibits activity against human CD39 with apparent Ki,app values of 14 μM.Ticlopidine inhibits recombinant human CD39 expressed in COS-7-cells with the Ki value of 127±12?μM.Growth rate is affected during the first days of culture, Ticlopidine (30 and 150 μM) reducing its effect in the following days.
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