40180-04-9

• 常用中文名：替宁酸
• 常用英文名：Tienilic acid
• CAS号：40180-04-9
• 分子式：C₁₃H₈Cl₂O₄S
• 分子量：331.17
• 相关类别： 研究领域 代谢疾病
• 发布时间：2018-06-11 15:19:40
• 更新时间：2024-01-06 13:22:56
• 铁粉酸是一种尿酸利尿剂。噻吩酸具有一定的肝毒性[1][3]。

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: 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

物化性质

• 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

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:
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
• 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.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AG9300000 CHEMICAL NAME : Acetic acid, (2,3-dichloro-4-(2-thienylcarbonyl)phenoxy)- CAS REGISTRY NUMBER : 40180-04-9 BEILSTEIN REFERENCE NO. : 1260086 LAST UPDATED : 199612 DATA ITEMS CITED : 10 MOLECULAR FORMULA : C13-H8-Cl2-O4-S MOLECULAR WEIGHT : 331.17 WISWESSER LINE NOTATION : T5SJ BVR BG CG DO1VQ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 3571 ug/kg TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - urine volume decreased TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 6666 ug/kg TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 5 mg/kg TOXIC EFFECTS : Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - urine volume decreased TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1275 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 318 mg/kg TOXIC EFFECTS : Kidney, Ureter, Bladder - urine volume increased TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 225 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3360 mg/kg/28D-I TOXIC EFFECTS : Vascular - BP lowering not characterized in autonomic section Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 6300 mg/kg/14D-I TOXIC EFFECTS : Liver - other changes Kidney, Ureter, Bladder - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) MUTATION DATA TYPE OF TEST : Mutation in mammalian somatic cells TEST SYSTEM : Rodent - hamster Lung DOSE/DURATION : 100 umol/L REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 157,1,1985

安全

• 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

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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%