< 生产厂家 价格 >

噻氯匹啶

噻氯匹啶用途

【用途一】
血小板膜稳定剂，有抑制血小板聚集，阻止血栓形成，降低血液粘稠度，改善微循环等作用。其作用优于阿司匹林、磺吡唑酮和潘生丁。用于血管手术和体外循环发生的血栓、动脉闭塞性脉管炎及闭塞性动脉硬化。可降低中风、心肌梗塞或血栓栓塞性中风的血管坏死发生率。
点击显示

噻氯匹啶名称

[ CAS 号 ]:
55142-85-3

[ 中文名 ]:
噻氯匹定

[ 英文名 ]:
Ticlopidine

[中文别名 ]:

[英文别名 ]:

噻氯匹啶生物活性

[ 描述 ]:

噻氯匹定(PCR 5332)是一种抗血栓前药,作为CD39的变构非竞争性抑制剂,IC50为81.7 µM.噻氯匹定阻断数种NTPDase同功酶,IC50为170 μM和149 对于NTPDase2和NTPDase3,分别为µM[1]。噻氯匹定是CYP2C19人肝细胞色素的抑制剂。噻氯匹定抑制CYP2C9和CYP3A4的IC50分别为26.0和32.3μM[2][3]。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450

[ 靶点 ]

Cytochrome P450[1]


[体外研究]

噻氯匹定具有抗人CD39的活性,表观Ki、app值为14µM[1]。噻氯匹定抑制在Ki值为127±12的COS-7细胞中表达的重组人CD39 µM[1]。生长速度在培养的第一天受到影响,噻氯匹定(30和150µM)会在接下来的几天降低其效果[4]。细胞增殖试验[4]细胞系：人内皮细胞浓度：30和150µM培养时间：2,6；10天的结果：与对照组相比,经处理的细胞生长较慢,这种效应与培养基中噻氯匹定的浓度有关。

[体内研究]

口服含10mg/kg噻氯匹定的氯沙坦可显著增加AUC(65.0%),表明噻氯匹定可有效抑制氯沙坦在肠道和/或肝脏中的代谢[3]。动物模型：雄性Sprague-Dawley大鼠(7-8周龄,体重270-300g)[3]剂量：4或10mg/kg给药：口服氯沙坦前30min口服。结果：口服氯沙坦和10mg/kg噻氯匹定后,氯沙坦的AUC和Cmax显著高于对照组大鼠(分别为65.0%和49.4%)。

[参考文献]

[1]. Laura Schäkel, et al. 2-Substituted thienotetrahydropyridine derivatives: Allosteric ectonucleotidase inhibitors. Arch Pharm (Weinheim). 2021 Dec;354(12):e2100300.

[2]. I.KRASLOVA1, et al. Ticlopidine-Induced Cholestatic Inflammatory Hepatitis: New Insights into Pathogenetic Mechanisms of Drug-Related Hepatotoxicity.

[3]. Si-hyung Yang, et al. Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats. Acta Pharmacol Sin. 2011 Jul;32(7):967-72.

[4]. F Piovella, et al. The effect of Ticlopidine on human endothelial cells in culture. Thromb Res. 1984 Feb 1;33(3):323-32.

噻氯匹啶物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
367.3±37.0 °C at 760 mmHg

[ 分子式 ]:
C14H14ClNS

[ 分子量 ]:
263.786

[ 闪点 ]:
175.9±26.5 °C

[ 精确质量 ]:
263.053558

[ PSA ]:
31.48000

[ LogP ]:
3.77

[ 外观性状 ]:
浅黄色固体

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.638

[ 储存条件 ]:
-20℃

噻氯匹啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XJ9089200
CHEMICAL NAME :
Thieno(3,2-c)pyridine, 4,5,6,7-tetrahydro-5-((2-chlorophenyl)methyl)-
CAS REGISTRY NUMBER :
55142-85-3
LAST UPDATED :
199712
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C14-H14-Cl-N-S
MOLECULAR WEIGHT :
263.80

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
336 mg/kg/47D-I
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - other changes Blood - agranulocytosis Blood - thrombocytopenia
REFERENCE :
APHRER Annals of Pharmacotherpy. (Harvey Whitney Books Co., POB 42696, Cincinnati, OH 45242) V. 26- 1992- Volume(issue)/page/year: 28,1236,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
600 mg/kg/60D-I
TOXIC EFFECTS :
Blood - aplastic anemia Blood - changes in bone marrow (not otherwise specified) Nutritional and Gross Metabolic - body temperature increase
REFERENCE :
IJMDAI Israel Journal of Medical Sciences. (POB 1435, Jerusalem 91013, Israel) V.1- 1965- Volume(issue)/page/year: 31,444,1995
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
429 mg/kg/6OD-I
TOXIC EFFECTS :
Gastrointestinal - hypermotility, diarrhea
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 1,407,1984
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
100 mg/kg/10D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - urine volume decreased Blood - eosinophilia
REFERENCE :
AJKDDP American Journal of Kidney Diseases. (Grune & Stratton, Inc., Journal Subscription Dept., POB 6280, Duluth, MN 55806) V.1- 1981- Volume(issue)/page/year: 25,934,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1780 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
70 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
600 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1250 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
88 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>6 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - pleural thickening Skin and Appendages - hair
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983
点击显示

噻氯匹啶安全信息

[ 危害码 (欧洲) ]:
C,Xi

[ 风险声明 (欧洲) ]:
R34:Causes burns.

[ 安全声明 (欧洲) ]:
S26-S27-S36/37/39-S45

[ 危险品运输编码 ]:
UN 3261 8/PG 3

[ WGK德国 ]:
3

[ 海关编码 ]:
2934999090

噻氯匹啶合成路线

详细合成路线

噻氯匹啶上下游产品

噻氯匹啶上游产品

噻氯匹啶下游产品

噻氯匹啶制备

噻吩溶于无水乙醚，在0℃缓慢滴加丁基锂乙醚溶液，再在室温搅拌。然后滴加环氧乙烷乙醚溶液，处理得2-羟乙基噻吩。将其溶于吡啶，在5℃以下分批加入对甲苯磺酰氯，室温搅拌，处理得磺酰化产物。该磺酰化产物和邻氯苄胺溶于甲苯，回流。滤除固体，滤液用盐酸提取。提取液浓缩，放置。沉淀用丙酮洗。然后将其与甲醛及水搅拌，回流，滤液用稀氢氧化钠碱化，异丙醚提取，经处理加入少许浓盐酸和丙酮，放置，析出结晶，即为盐酸噻氯匹定。
点击显示

噻氯匹啶海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

相关药品：

推荐生产厂家/供应商：

公司名：上海创赛科技有限公司

区域：上海市嘉定区

价格：
￥988.0/100mg ￥441.0/25mg ￥122.0/5mg

联系人：夏言

产品详情：[Perfemiker]噻氯匹啶,95%

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥104.9/5mg ￥449.9/1ml ￥388.9/25mg ￥879.0/250mg

联系人：阿拉丁李高志

产品详情：噻氯匹啶

公司名：广东翁江化学试剂有限公司

区域：韶关市翁源县

价格：
￥2800.0/1g

联系人：朱丽丹

产品详情：噻氯匹啶

查看所有供应商请点击：

噻氯匹啶供应商

热门化合物

【噻氯匹啶】化源网提供噻氯匹啶CAS号55142-85-3，噻氯匹啶MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询噻氯匹啶上化源网，专业又轻松。>>电脑版：噻氯匹啶

标题：噻氯匹啶_用途_密度_沸点_噻氯匹啶CAS号【55142-85-3】_化源网 地址：https://m.chemsrc.com/mip/cas/55142-85-3_27756.html