122-06-5

• 常用中文名：司替巴脒
• 常用英文名：Stilbamidine
• CAS号：122-06-5
• 分子式：C₁₆H₁₆N₄
• 分子量：264.32500
• 相关类别： 信号通路 抗感染 真菌
• 发布时间：2016-01-09 01:30:55
• 更新时间：2024-01-16 20:51:55
• Stilbamidine 是 Stilbene 衍生的二脒化合物,主要以其羟乙基磺酸盐形式发挥作用,用于治疗各种真菌感染。

名称

• 中文名: 司替巴脒
• 英文名: 2-(2-phenylethenyl)benzenecarboximidamide
• 英文别名: Stilbamidin; Benzenecarboximidamide,4,4'-(1,2-ethenediyl)bis; 4,4'-Vinylenedi(benzamidine); stilbamidine; trans-stilbene-4,4'-dicarboxamidine; trans-Stilben-4,4'-dicarbamidin; trans-Stilben-dicarbamidin-(4.4'); 4,4'-Stilbenedicarboxamidine(7CI,8CI)

物化性质

• 密度: 1.19g/cm3
• 沸点: 456.4ºC at 760mmHg
• 分子式: C₁₆H₁₆N₄
• 分子量: 264.32500
• 闪点: 229.8ºC
• 精确质量: 264.13700
• PSA: 99.74000
• LogP: 4.02520
• 蒸汽压: 1.62E-08mmHg at 25°C
• 折射率: 1.634
• 储存条件: 2-8℃

生物活性

• 描述: Stilbamidine 是 Stilbene 衍生的二脒化合物,主要以其羟乙基磺酸盐形式发挥作用,用于治疗各种真菌感染。
• 相关类别:
  信号通路 >> 抗感染 >> 真菌
  研究领域 >> 感染
  研究领域 >> 癌症
• 靶点:

  fungal

• 体外研究: 高亲和性喷他脒转运蛋白(HAPT1)被Propamidine抑制,但对Stilbamidine仅表现出低亲和力。相反,腺苷敏感的喷他脒转运蛋白(ASPT1)被Stilbamidine和Propamidine强烈抑制。 [3H]喷他脒摄取是在各种浓度的腺苷(IC50 =1.2μM)或氧化melarsen(IC50 =0.7μM)存在下,以及在250μM腺苷和浓度升高的次黄嘌呤,丙胺脒(IC50)存在下测定的。 =6.1μM)和Stilbamidine(IC50 =110μM)[1]。两种二脒化合物,Stilbamidine和Pentamidine用于治疗多发性骨髓瘤,这是一种常常发生血清中球蛋白含量增加的疾病[2]。
• 参考文献:

  [1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92.

  [2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : WJ5250000 CHEMICAL NAME : 4,4'-Stilbenedicarboxamidine CAS REGISTRY NUMBER : 122-06-5 BEILSTEIN REFERENCE NO. : 3206434 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C16-H16-N4 MOLECULAR WEIGHT : 264.36 WISWESSER LINE NOTATION : MUYZR D1U1R DYZUM HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - man DOSE/DURATION : 39 mg/kg/29D TOXIC EFFECTS : Behavioral - hallucinations, distorted perceptions Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - nausea or vomiting TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 43 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 : 115 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 : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 125 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 : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 30 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 - hamster DOSE/DURATION : 150 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value MUTATION DATA TYPE OF TEST : Mutation in microorganisms TEST SYSTEM : Yeast - Saccharomyces cerevisiae DOSE/DURATION : 190 umol/L REFERENCE : EJCODS European Journal of Cancer and Clinical Oncology. (Pergamon Press, c/o Elsevier Science, 660 White Plains Rd., Tarrytown, NY 10591) V.17(7)- 25, 1981-89. For publisher information, see EJCAEL Volume(issue)/page/year: 19,1575,1983

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