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2-氨基-6-苄基-4,5,6,7-四氢噻吩并[2,3-c]吡啶-3-甲酸乙酯

用途

替诺瑞定(Y-3642)是一种口服活性非甾体抗炎剂,具有较强的抗氧化能力和自由基清除剂活性。替诺瑞定通过抑制COX酶发挥作用,参与肝毒性抑制。[1][2][3].

名称

[ CAS 号 ]:
24237-54-5

[ 中文名 ]:
2-氨基-6-甲基-4,5,6,7-四噻吩[2,3-C]吡啶-3-甲酸乙酯

[ 英文名 ]:
Tinoridine

[中文别名 ]:

替诺立定

[英文别名 ]:

Dimaten
Tinoridine
Y 3642

生物活性

[ 描述 ]:

替诺瑞定(Y-3642)是一种口服活性非甾体抗炎剂,具有较强的抗氧化能力和自由基清除剂活性。替诺瑞定通过抑制COX酶发挥作用,参与肝毒性抑制。[1][2][3].

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

[体外研究]

替诺瑞定(10-100μM)对大鼠肝脏和肾脏溶酶体以及肝实质细胞的稳定性有影响[3]。替诺瑞定(1、10和100μM；30分钟)抑制体外肝赖氨酸自发释放酸性磷酸酶[3]。

[体内研究]

替诺瑞定(100 mg/kg；口服；单剂量)可抑制大鼠的CCl4肝毒性,对CCl4诱导的酶活性有很强的控制作用[2]。替诺瑞定(100 mg/kg；i.p.；单剂量)在体内保护大鼠肝脏和肾脏溶酶体的稳定性[3]。动物模型：雄性Wistar大鼠(180-220 g)[2]剂量：100 mg/kg给药：口服灌胃；单剂量；结果：抑制了CCl4诱导的血清谷氨酸-草酰乙酸转氨酶和谷氨酸-丙酮酸转氨酶活性的升高,并挽救了肝微粒体细胞色素p-450和葡萄糖-6-磷酸酶活性。

物理化学性质

[ 密度 ]:
1.256 g/cm3

[ 沸点 ]:
493.5ºC at 760 mmHg

[ 熔点 ]:
112-113ºC

[ 分子式 ]:
C₁₇H₂₀N₂O₂S

[ 分子量 ]:
316.41800

[ 精确质量 ]:
316.12500

[ PSA ]:
83.80000

[ LogP ]:
3.58440

[ 蒸汽压 ]:
7E-10mmHg at 25°C

[ 储存条件 ]:
室温

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ9088300

CHEMICAL NAME :: Thieno(2,3-c)pyridine-3-carboxylic acid, 4,5,6,7-tetrahydro-2-amino-6-benzyl-, ethyl ester

CAS REGISTRY NUMBER :: 24237-54-5

LAST UPDATED :: 199706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C17-H20-N2-O2-S

MOLECULAR WEIGHT :: 316.45

WISWESSER LINE NOTATION :: T56 BS HN&TJ CZ DVO2 H1R

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,998,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,998,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,998,1970

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,998,1970

安全信息

[ 海关编码 ]:
2934999090

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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%