87771-40-2

• 常用中文名：碘氟醇
• 常用英文名：Ioversol
• CAS号：87771-40-2
• 分子式：C₁₈H₂₄I₃N₃O₉
• 分子量：807.111
• 相关类别： 原料药 诊断用药 影象检查用药
• 发布时间：2018-08-10 18:17:25
• 更新时间：2024-01-02 21:08:44
• Ioversol 是一种非离子碘化造影剂。

名称

• 中文名: 碘氟醇
• 英文名: 1-N,3-N-bis(2,3-dihydroxypropyl)-5-[(2-hydroxyacetyl)-(2-hydroxyethyl)amino]-2,4,6-triiodobenzene-1,3-dicarboxamide
• 中文别名: N,N'-双(2,3-二羟基丙基)-5-[(2-羟基乙酰基)-(2-羟乙基)氨基]-2,4,6-三碘苯-1,3-二甲酰胺
• 英文别名: Ioversolum [Latin]; N,N'-bis(2,3-dihydroxypropyl)-5[(hydroxyacetyl)-(2-hydroxyethyl)-amino]-2,4,6-triiodo-1,3-benzenedicarboxamide; N,N'-Bis(2,3-dihydroxypropyl)-5-[(hydroxyacetyl)(2-hydroxyethyl)amino]-2,4,6-triiodbenzol-1,3-dicarboxamid; Optiray 160; UNII-N3RIB7X24K; N,N'-bis(2,3-dihydroxypropyl)-5-[(hydroxyacétyl)(2-hydroxyéthyl)amino]-2,4,6-triiodobenzène-1,3-dicarboxamide; Optiray; N,N'-bis(2,3-dihydroxypropyl)-5-[(hydroxyacetyl)(2-hydroxyethyl)amino]-2,4,6-triiodobenzene-1,3-dicarboxamide; MP-328; Optiray 320; [N,N'-bis-(2,3-dihydroxypropyl)-5-[(2-hydroxyacetyl)(2-hydroxyethyl)amino]-2,4,6-triiodoisophthalamide]; Optiray 350; N,N'-bis(2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl)glycolamido]-2,4,6-triiodoisophthalamide; Optiray 240; 1,3-Benzenedicarboxamide, N,N-bis(2,3-dihydroxypropyl)-5-[(2-hydroxyacetyl)(2-hydroxyethyl)amino]-2,4,6-triiodo-; 1,3-benzenedicarboxamide, N,N'-bis(2,3-dihydroxypropyl)-5-[(hydroxyacetyl)(2-hydroxyethyl)amino]-2,4,6-triiodo-; Ioversol; MFCD00867959; N,N'-Bis(2,3-dihydroxypropyl)-5-[glycoloyl(2-hydroxyethyl)amino]-2,4,6-triiodoisophthalamide

物化性质

• 密度: 2.3±0.1 g/cm3
• 沸点: 864.9±65.0 °C at 760 mmHg
• 熔点: 180-182ºC
• 分子式: C₁₈H₂₄I₃N₃O₉
• 分子量: 807.111
• 闪点: 476.9±34.3 °C
• 精确质量: 806.864624
• PSA: 199.89000
• LogP: -4.01
• 蒸汽压: 0.0±0.3 mmHg at 25°C
• 折射率: 1.739
• 储存条件: Refrigerator

生物活性

• 描述: Ioversol 是一种非离子碘化造影剂。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 其他
• 体外研究: Ioversol(100mg碘/ ml)暴露诱导NRK-52E细胞中乳酸脱氢酶释放显着增加和3-(4,5-二甲基二唑-2-基)-2,5-二苯基四唑溴化物转化减少。 Ioversol显着增加暴露于ioversol的NRK-52E细胞中凋亡和caspase-3蛋白表达4小时。 Ioversol处理诱导[Ca2 +] i和细胞内ROS的显着增加[1]。
• 体内研究: 与碘酞酸盐相比,碘佛醇具有极大降低的刺激内皮素释放的倾向,从培养的细胞和注射到麻醉的大鼠中。在对照组和USIC大鼠中,Ioversol产生的肾血管收缩作用少于碘酞酸,并且通过肌酐清除率和肾髓质形态学损伤评估的放射性对比肾病的发展在很大程度上得到了避免[2]。
• 细胞实验: 通过使用MTT摄取测定评估细胞活力。 MTT（一种四唑盐）转化为甲is取决于一组线粒体脱氢酶的活性，因此是细胞代谢活性的指标。用分光光度计在570nm的波长下测量MTT四唑盐的颜色。简而言之，在除去培养基后加入新鲜的MTT溶液（在1×PBS中10mg / mL）（1:20体积的培养基）并将细胞温育1.5小时。裂解细胞，通过与MTT裂解缓冲液一起温育过夜，将紫色甲crystals溶解到溶液中。结果表示为未损伤的对照细胞的百分比，假设对照孔的吸光度为100％。
• 参考文献:

  [1]. Yang D, et al. Selective inhibition of the reverse mode of Na(+)/Ca(2+) exchanger attenuates contrast-induced cell injury. Am J Nephrol. 2013;37(3):264-73. doi: 10.1159/000348526. Epub 2013 Mar 13.

  [2]. Heyman SN, et al. Effects of ioversol versus iothalamate on endothelin release and radiocontrast nephropathy. Invest Radiol. 1993 Apr;28(4):313-8.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : CZ2229000 CHEMICAL NAME : 1,3-Benzenedicarboxamide, N,N'-bis(2,3-dihydroxypropyl)-5-((hydroxyacetyl)(2-hy droxyethyl) amino)-2,4,6-triiodo- CAS REGISTRY NUMBER : 87771-40-2 LAST UPDATED : 199612 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C18-H24-I3-N3-O9 MOLECULAR WEIGHT : 807.15 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 : 21200 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: 44,1275,1994 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intracerebral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1314 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,769,1994 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Parenteral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 833 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 22,769,1994 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 38372 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - respiratory depression Liver - other changes Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) REFERENCE : YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 20,1127,1992 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 19 gm/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating - 20 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : INVRAV Investigative Radiology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1966- Volume(issue)/page/year: 24(Suppl 1),S16,1989 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 28800 mg/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 4 day(s) post-birth TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) REFERENCE : INVRAV Investigative Radiology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1966- Volume(issue)/page/year: 24(Suppl 1),S16,1989

安全

• 危险品运输编码: NONH for all modes of transport

合成路线

77868-40-7 107-07-3 ~% 87771-40-2

文献：WO2008/104853 A1, ; Page/Page column 15; 11-12 ;

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