替宁酸

更新时间:2024-01-06 13:22:56

替宁酸结构式
替宁酸结构式
品牌特惠专场
常用名 替宁酸 英文名 Tienilic acid
CAS号 40180-04-9 分子量 331.17
密度 1.5±0.1 g/cm3 沸点 534.6±50.0 °C at 760 mmHg
分子式 C13H8Cl2O4S 熔点 148-149ºC
MSDS 中文版 美版 闪点 277.1±30.1 °C

 替宁酸用途


铁粉酸是一种尿酸利尿剂。噻吩酸具有一定的肝毒性[1][3]。

 替宁酸名称

中文名 替宁酸
英文名 tienilic acid
中文别名 2,3-二氯-4-(2-噻吩甲酰基)苯氧基乙酸 | 噻吩利尿酸 | 2-(2,3-二氯-4-(噻吩-2-羰基)苯氧基)乙酸
英文别名 更多

 替宁酸生物活性

描述 铁粉酸是一种尿酸利尿剂。噻吩酸具有一定的肝毒性[1][3]。
相关类别
体内研究 Tienilic acid(大鼠和小鼠为100 mg/lg,猪和狗为5 mg/kg;PO和IV;单次剂量)仅存在于血浆中,通过胆汁和尿液禁食消除,在不同物种中表现出微小差异【2】。替尼酸(0-480 mg/kg;PO;持续28天)可降低血压、血清、尿酸血红蛋白,并增加S-GPT;诱导小群肝细胞的单细胞坏死[3]。动物模型:大鼠、小鼠、猪和狗【2】剂量:大鼠和小鼠100 mg/lg,猪和狗5 mg/kg给药:PO和IV;单次给药结果:仅在血液水平与血浆蛋白有重要结合的血浆中发现;药理作用数小时;在给药后的前48小时内,通过胆道,尤其是尿路禁食,几乎完全消除;在不同物种中测量的参数只有很小的差异。动物模型:雌性和雄性Sprague-Dawley大鼠【3】剂量:0、30、120和480 mg/kg给药:PO;28天结果:30 mg/kg时血压和血尿酸降低;在120和480 mg/kg时,血红蛋白略有下降,S-GPT升高;显著增加雄性大鼠的肝脏重量和血清镁浓度,而雌性大鼠的肝脏重量仅略有增加;此外,诱导小群肝细胞单细胞坏死。
参考文献

[1]. Lemieux G, et al, Baverel G. Metabolic effects in man of tienilic acid, a new diuretic with uricosuric properties. Nephron. 1978;20(1):54-64.

[2]. Levron, J.C., et al. Pharmacokinetic study of 2,3-dichloro 4- (2-thienyl keto14C) phenoxyacetic acid (tienilic acid) in animals. European Journal of Drug Metabolism and Pharmacokinetics 2, 107–120 (1977).

[3]. Oker-Blom C, et al. Toxicological studies on tienilic acid in rats. Toxicol Lett. 1980;6(2):93-99.

 替宁酸物理化学性质

密度 1.5±0.1 g/cm3
沸点 534.6±50.0 °C at 760 mmHg
熔点 148-149ºC
分子式 C13H8Cl2O4S
分子量 331.17
闪点 277.1±30.1 °C
精确质量 329.952026
PSA 91.84000
LogP 3.07
蒸汽压 0.0±1.5 mmHg at 25°C
折射率 1.632
储存条件 -20°C

 替宁酸毒性和生态

 替宁酸安全信息

危害码 (欧洲) Xi
危险品运输编码 NONH for all modes of transport
RTECS号 AG9300000
海关编码 2934999090

 替宁酸上下游产品

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 替宁酸海关

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%

 替宁酸文献28

更多文献
Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.

Expert Opin. Drug Metab. Toxicol. 10(10) , 1313-24, (2014)

Drug resistance by Plasmodium falciparum remains a challenge in malaria chemotherapy. This paper will focus on physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hy...

Coupling Laser Diode Thermal Desorption with Acoustic Sample Deposition to Improve Throughput of Mass Spectrometry-Based Screening.

J. Biomol. Screen. 21 , 165-75, (2016)

The move toward label-free screening in drug discovery has increased the demand for mass spectrometry (MS)-based analysis. Here we investigated the approach of coupling acoustic sample deposition (ASD...

Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose.

Chem. Res. Toxicol. 21(9) , 1814-22, (2008)

In vitro covalent binding assessments of drugs have been useful in providing retrospective insights into the association between drug metabolism and a resulting toxicological response. On the basis of...

 替宁酸英文别名

Tienilic acid
(2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy)acetic acid
Tienilico acido
(2,3-Dichloro-4-(2-thiophenecarbonyl)phenoxy)acetic acid
Acidum tienilicum
TienilicAcid
Selacryn
acetic acid, [2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-
Diflurex
Ticrynafen Tienylic acid [2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy]-acetic acid
[2,3-dichloro-4-(2-thenoyl)phenoxy]acetic acid
Acido tienilico
Acide tienilique
2,3-dichloro-4-(thien-2-ylcarbonyl)-phenoxyacetic acid
[2,3-dichloro-4-(thiophene-2-carbonyl)-phenoxy]-acetic acid
[2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy]acetic acid
Acetic acid, 2-[2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-
Ticrex
{[2,3-dichloro-4-(2-thienylcarbonyl)phenyl]oxy}acetic acid
Ticrynafen
2-[2,3-dichloro-4-(thiophene-2-carbonyl)phenoxy]acetic acid
Thienylic acid
[2,3-dichloro-4-(thiophen-2-ylcarbonyl)phenoxy]acetic acid
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