492-18-2

• 常用中文名：汞撒利
• 常用英文名：mersalyl
• CAS号：492-18-2
• 分子式：C₁₃H₁₆HgNNaO₆
• 分子量：505.84900
• 相关类别： 原料药 泌尿系统用药 利尿药
• 发布时间：2018-08-11 14:07:51
• 更新时间：2024-01-14 17:51:18
• Mersalyl(Salirgan)是一种有效的血管内皮生长因子(VEGF)和缺氧诱导因子1(HIF-1)诱导剂。美沙利诱导VEGF和ENO1 mRNA表达。美沙利具有利尿作用[1][2][3]。

名称

• 中文名: 汞撒利
• 英文名: sodium,[3-[[2-(carboxylatomethoxy)benzoyl]amino]-2-methoxypropyl]mercury,hydrate
• 英文别名: Mercusal; Mersalyl acid sodium salt; Salyrgan; Diursal; Mercurital; Mersalyl; Igrosin; Mercuramide; Sodium mersalyl

物化性质

• 分子式: C₁₃H₁₆HgNNaO₆
• 分子量: 505.84900
• 精确质量: 507.05800
• PSA: 103.24000

生物活性

• 描述: Mersalyl(Salirgan)是一种有效的血管内皮生长因子(VEGF)和缺氧诱导因子1(HIF-1)诱导剂。美沙利诱导VEGF和ENO1 mRNA表达。美沙利具有利尿作用[1][2][3]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> HIF/HIF脯氨酰-羟化酶
  研究领域 >> 代谢疾病
  信号通路 >> 蛋白酪氨酸激酶 >> VEGFR
• 体外研究: 美沙利(100µM)诱导VEGF和ENO1 mRNA表达,但抑制缺氧、DFO或CoCl2诱导的EPO mRNA表达[2]。Mersalyl(20µM；5分钟)是一种不透细胞的有机汞化合物,与线粒体膜蛋白中的游离巯基反应[1]。RT-PCR[2]细胞系：Hep3B细胞浓度：100µM孵育时间：6 h结果：诱导VEGF和ENO1 mRNA表达,但抑制缺氧、DFO或CoCl2诱导的EPO mRNA表达。
• 体内研究: 美沙利(2.5-40mg/kg；肌肉注射)对大鼠有利尿作用[3]。动物模型：大鼠[3]剂量：2.5-40mg/kg给药：肌肉注射结果：5 mg/kg时巯基浓度显著降低。
• 参考文献:

  [1]. Kowaltowski AJ, et al. Mitochondrial membrane protein thiol reactivity with N-ethylmaleimide or mersalyl is modified by Ca2+: correlation with mitochondrial permeability transition. Biochim Biophys Acta. 1997 Feb 15;1318(3):395-402.

  [2]. Agani F, et al. Mersalyl is a novel inducer of vascular endothelial growth factor gene expression and hypoxia-inducible factor 1 activity. Mol Pharmacol. 1998 Nov;54(5):749-54.

  [3]. FARAH A, et al. Histochemical studies on the site of action of mercurial diuretics. J Histochem Cytochem. 1955 Jul;3(4):271-3.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : OV7875000 CHEMICAL NAME : Mercury, 3-(alpha-carboxy-o-anisamido)-2-methoxypropyl hydroxy-, monosodium salt CAS REGISTRY NUMBER : 492-18-2 LAST UPDATED : 199712 DATA ITEMS CITED : 26 MOLECULAR FORMULA : C13-H16-Hg-N-O6.Na MOLECULAR WEIGHT : 505.88 WISWESSER LINE NOTATION : QV1OR BVM1YO1&1-HG-Q &-NA- HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 17700 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 24 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 118 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JOCEAH Journal of Organic Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1936- Volume(issue)/page/year: 16,1879,1951 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 72600 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 7 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 152,341,1930 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 24500 ug/kg REFERENCE : JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951 *** REVIEWS *** ACGIH TLV-TWA 0.1 mg(Hg)/m3 (skin) DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 *** U.S. STANDARDS AND REGULATIONS *** MSHA STANDARD-air:TWA 0.05 mg(Hg)/m3 DTLWS* "Documentation of the Threshold Limit Values for Substances in Workroom Air," Supplements. For publisher information, see 85INA8. Volume(issue)/page/year: 3,22,1973 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-AUSTRALIA:TWA 0.05 mg(Hg)/m3;Skin JAN 1993 OEL-BELGIUM:TWA 0.05 mg(Hg)/m3;Skin JAN 1993 OEL-DENMARK:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-FINLAND:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-FRANCE:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-GERMANY:TWA 0.01 ppm (0.1 mg(Hg)/m3) JAN 1993 OEL-HUNGARY:TWA 0.02 mg(Hg)/m3;STEL 0.04 mg(Hg)/m3 JAN 1993 OEL-JAPAN:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-THE NETHERLANDS:TWA 0.05 mg(Hg)/m3;STEL 0.15 mg(Hg)/m3 JAN 1993 OEL-THE PHILIPPINES:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-POLAND:TWA 0.01 mg(Hg)/m3 JAN 1993 OEL-RUSSIA:TWA 0.05 mg(Hg)/m3;STEL 0.01 mg(Hg)/m3 JAN 1993 OEL-SWEDEN:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-THAILAND:STEL 0.05 mg(Hg)/m3 JAN 1993 OEL-UNITED KINGDOM:TWA 0.05 mg(Hg)/m3;STEL 0.15 mg(Hg)/m3 JAN 1993 OEL IN BULGARIA, COLOMBIA, JORDAN, KOREA check ACGIH TLV OEL IN NEW ZEALAND, SINGAPORE, VIETNAM check ACGIH TLV *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH RECOMMENDED EXPOSURE LEVEL (REL) : NIOSH REL TO MERCURY, ARYL AND INORGANIC-air:CL 0.1 mg/m3 (Sk) REFERENCE : NIOSH* National Institute for Occupational Safety and Health, U.S. Dept. of Health, Education, and Welfare, Reports and Memoranda. Volume(issue)/page/year: DHHS #92-100,1992

安全

• 危险品运输编码: UN 2025
• 包装等级: II
• 危险类别: 6.1(a)