Ticlopidine

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Ticlopidine

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CAS NO:

55142-85-3

PCR 5332

Ticlopidine (PCR 5332) 是一种抗血栓前药，作为非竞争性的变构CD39抑制剂，IC₅₀为 81.7 μM。Ticlopidine 阻断 NTPDase 同工酶，对NTPDase2和NTPDase3的IC₅₀分别为 170 μM 和 149 μM。Ticlopidine 是CYP2C19人肝细胞色素的抑制剂。Ticlopidine 抑制 CYP2C9 和 CYP3A4，IC₅₀值分别为 26.0 和 32.3 μM。

生物活性

Ticlopidine (PCR 5332), an antithrombotic prodrug, acts as an allosteric, noncompetitive inhibitor ofCD39with theIC₅₀of 81.7 μM. Ticlopidine blocks severalNTPDaseisoenzymes withIC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively^[1]. Ticlopidine is an inhibitor ofCYP2C19human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 withIC₅₀s of 26.0 and 32.3 μM, respectively^[2]^[3].

IC₅₀& Target

Cytochrome P450^[1]

体外研究
(In Vitro)

Ticlopidine exhibits activity against human CD39 with apparent K_i,appvalues of 14 μM^[1].
Ticlopidine inhibits recombinant human CD39 expressed in COS-7-cells with the K_ivalue 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].

Cell Proliferation Assay^[4]

Cell Line:	Human endothelial cells
Concentration:	30 and 150 μM
Incubation Time:	2, 6; 10 days
Result:	Treated cells grow slower if compared with controls and this effect correlates with the concentration of Ticlopidine in the culture medium.

体内研究
(In Vivo)

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^[3].

Animal Model:	Male Sprague-Dawley rats (7-8 weeks old, weighing 270-300 g)^[3]
Dosage:	4 or 10 mg/kg
Administration:	Orally administered 30 min before oral administration of losartan.
Result:	The AUC and C_maxof 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.

Clinical Trial

分子量

263.79

Formula

C₁₄H₁₄ClNS

CAS 号

55142-85-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.