Ticlopidine hydrochloride
(Synonyms: 盐酸噻氯匹定) 目录号 : GC65614
A P2Y12 receptor antagonist with antiplatelet activity
Cas No.:53885-35-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ticlopidine is a thienopyridine P2Y12 receptor antagonist.1 It inhibits aggregation of human platelets induced by collagen, arachidonic acid , and ADP .2 It also inhibits ADP-induced aggregation of rat platelets and decreases thrombus weight in vivo in a rat model of arterio-venous shunt thrombosis when administered at a dose of 100 mg/kg.3 Ticlopidine (300 mg/kg) inhibits healing of acetic acid-induced gastric ulcers in rats.4 Formulations containing ticlopidine have been used in the prevention of thrombotic stroke.
1.Porto, I., Giubilato, S., De Maria, G.L., et al.Platelet P2Y12 receptor inhibition by thienopyridines: Status and futureExpert Opin. Investig. Drugs18(9)1317-1332(2009) 2.Bruno, J.J.The mechanisms of action of ticlopidineThromb. Res. Suppl.459-67(1983) 3.Sugidachi, A., Asai, F., Ogawa, T., et al.The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist propertiesBr. J. Pharmacol.129(7)1439-1446(2000) 4.Ma, L., Elliott, S.N., Cirino, G., et al.Platelets modulate gastric ulcer healing: Role of endostatin and vascular endothelial growth factor releaseProc. Natl. Acad. Sci. USA98(11)6470-6475(2001)
| Cas No. | 53885-35-1 | SDF | Download SDF |
| 别名 | 盐酸噻氯匹定 | ||
| 分子式 | C14H15Cl2NS | 分子量 | 300.25 |
| 溶解度 | DMSO : 50 mg/mL (166.53 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3306 mL | 16.6528 mL | 33.3056 mL |
| 5 mM | 0.6661 mL | 3.3306 mL | 6.6611 mL |
| 10 mM | 0.3331 mL | 1.6653 mL | 3.3306 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Ticlopidine hydrochloride
J Neurosci Nurs 1992 Oct;24(5):296-300.PMID:1402156DOI:10.1097/01376517-199210000-00012.
Ticlopidine, a new prototype antiplatelet agent, offers a significant alternative in the primary and secondary prevention of atherothrombotic stroke. While 2 multicenter trials demonstrated benefits of ticlopidine, this drug is not without risks and limitations and more studies are indicated. The neuroscience nurse must apply current knowledge about ticlopidine in the care for patients receiving ticlopidine therapy.
Ticlopidine hydrochloride: relationship between dose, kinetics, plasma concentration and effect on platelet function
Thromb Res Suppl 1983;4:119-28.PMID:6356462DOI:10.1016/0049-3848(83)90367-5.
This is a review of the available data about the pharmacodynamic profile of ticlopidine in man in relation to its pharmacokinetic and metabolic characteristics. There is a rapid dose-dependent onset of effect on platelet function and a time-dependent effect on bleeding. The ticlopidine effect appears to be due to the direct action on circulating platelets. The contributions of a metabolite, a 2-keto derivative, is also discussed.
Ticlopidine hydrochloride use and threatened stroke
West J Med 1994 Jan;160(1):43-7.PMID:8128701doi
Ticlopidine hydrochloride is an antiplatelet agent of proven antithrombotic efficacy that in December 1991 became available for general clinical use in the United States. The relative value of ticlopidine compared with aspirin, also an effective antiplatelet agent, has become a key clinical issue. Whereas ticlopidine is somewhat more effective than aspirin for preventing stroke in certain populations, it is also more expensive and potentially toxic. We recommend its use for patients with threatened stroke who are intolerant of aspirin and for patients who have cerebral ischemic symptoms despite aspirin therapy. Patients surviving major ischemic stroke make up a third group for whom ticlopidine use may be recommended in preference to aspirin. The use of ticlopidine rather than aspirin in patients with other cerebrovascular conditions is not strongly supported by existing data. The risk-benefit-cost equation involving ticlopidine versus other antithrombotic therapies is complex, rendering a wide range of acceptable management practices. If reliable laboratory monitoring for neutropenia during the first 3 months of therapy is not feasible, ticlopidine should not be used.
Electroencephalographical effects of sarpogrelate hydrochloride versus Ticlopidine hydrochloride in elderly patients with peripheral atherosclerosis
J Int Med Res 2004 May-Jun;32(3):274-83.PMID:15174221DOI:10.1177/147323000403200307.
The aim was to determine the efficacy of sarpogrelate (a selective 5-hydroxytryptamine-2-serotonergic receptor antagonist) on cerebrovascular function and mean blood pressure (mBP) in elderly patients (> 60 years old). Patients with peripheral circulatory disorders were studied using electroencephalogram (EEG) and mBP measurements before and after 2 years' treatment with either sarpogrelate (n = 31) or ticlopidine (n = 43). Ticlopidine had no significant effect on the whole brain. Sarpogrelate decreased the percentage of slow waves (%slow), but not significantly, and was associated with a smaller change in the percentage of slow waves (delta slow). In the anterior area, neither drug caused significant EEG changes. In the posterior area, sarpogrelate significantly decreased the %slow and increased the %alpha values, and was associated with a significantly higher delta alpha value than ticlopidine. The results suggest that sarpogrelate hydrochloride can suppress serotonin-induced pathological processes in peripheral circulatory disorders and may be recommended as an anti-platelet agent, even in elderly patients with subclinical arteriosclerosis.
Quantitative determination of Ticlopidine hydrochloride in human plasma by high-performance liquid chromatography-electronspray ionization mass spectrometry
Arzneimittelforschung 2009;59(3):121-8.PMID:19402342DOI:10.1055/s-0031-1296374.
A sensitive, selective and simple high performance liquid chromatographyelectrospray ionization-mass spectrometry (HPLC-ESI-MS) was developed and validated for the quantification of Ticlopidine hydrochloride (CAS 53885-35-1) in human plasma using loratadine (CAS 79794-75-5) as internal standard (IS). Following liquid-liquid extraction, the analyte and the IS were extracted from plasma samples by n-hexane:isopropanol (95:5, v/v), separated by HPLC on a commercially available column (150 mm x 2.0 mm ID, 5 microm) with a mobile phase of acetonitrile: 10 mmol/L ammonium acetate buffer solution (85:15, v/v) and analyzed on a quadrupole mass spectrometer with ESI interface operating in the positive-ion mode. The correlation coefficient of the calibration curve was linear (r2 > 0.99) over the concentration range of 1-1000 ng/mL for Ticlopidine hydrochloride. The intra- and inter-batch precisions were less than 15% of the relative standard deviation and the accuracy ranged from 85 to 115% in terms of percent accuracy. The limit of detection (LOD) of Ticlopidine hydrochloride was 0.5 ng/mL. The extraction recovery of Ticlopidine hydrochloride was more than 80%. The proposed method enables the unambiguous identification and quantification of Ticlopidine hydrochloride for pharmacokinetic, bioavailability or bioequivalence studies.