Ticlopidine (hydrochloride)

Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively^[1][2][3][4]. In Vitro:Ticlopidine hydrochloride exhibits activity against human CD39 with apparent K_i,app values of 14 µM^[1].
Ticlopidine hydrochloride inhibits recombinant human CD39 expressed in COS-7-cells with the K_i value of 127 µM^[1].
Growth rate is affected during the first days of culture, Ticlopidine (30 and 150 µM) hydrochloride reducing its effect in the following days^[4]. In Vivo:Oral administration of Losartan (HY-17512) 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^[3].