Ticlopidine HCl

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Chemical Structure| 53885-35-1 同义名 : 噻氯匹定盐酸盐 ;Ticlopidine (hydrochloride);Ticlopidine hydrochloride
CAS号 : 53885-35-1
货号 : A218498
分子式 : C14H15Cl2NS
纯度 : 99%
分子量 : 300.247
MDL号 : MFCD00079606
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(166.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(166.53 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 80 mg/mL suspension

生物活性
靶点

  • P2 receptor

    P2 receptor, IC50:~2 μM
描述 Ticlopidine Hydrochloride is a hydrochloride form of Ticlopidine. Ticlopidine is a selective and the first FDA-approved P2Y12 antagonist which can affect platelet aggregation when. It can be metabolized through cytochrome P450 in the liver and forms the active thienopyridine metabolites. The thienopyridine metabolites can irreversibly antagonize the P2Y12 receptor[3]. This results in inhibition of the binding of the P2Y12 agonist 2-methylthio-ADP and the ADP-induced downregulation of adenylyl cyclase[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01381185 Acute Myocardial Infarction Phase 4 Completed - Czech Republic ... 展开 >> University Hospital Ostrava Ostrava, Poruba, Czech Republic, 70852 Departement of Laboratory Medicine, Prostejov Hospital Prostejov, Czech Republic, 79604 收起 <<
NCT01448330 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Samsung medical center Seoul, Korea, Republic of 收起 <<
NCT01469416 Healthy Phase 1 Completed - United States, California ... 展开 >> Clinical Research Center, UCSF San Francisco, California, United States, 94143 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.65mL

3.33mL

1.67mL

33.31mL

6.66mL

3.33mL
参考文献

[1]Michelson AD, et al. P2Y12 antagonism: promises and challenges. Arterioscler Thromb Vasc Biol. 2008 Mar;28(3):s33-8.

[2]Savi P, Herbert JM, et al. Clopidogrel and ticlopidine: P2Y12 adenosine diphosphate-receptor antagonists for the prevention of atherothrombosis. Semin Thromb Hemost. 2005 Apr;31(2):174-83.

[3]Michelson AD. P2Y12 antagonism: promises and challenges. Arterioscler Thromb Vasc Biol. 2008 Mar;28(3):s33-8. doi: 10.1161/ATVBAHA.107.160689. Epub 2008 Jan 3. PMID:18174449.

[4]Savi P, Herbert JM. Clopidogrel and ticlopidine: P2Y12 adenosine diphosphate-receptor antagonists for the prevention of atherothrombosis. Semin Thromb Hemost. 2005 Apr;31(2):174-83. doi: 10.1055/s-2005-869523. PMID: 15852221.