Bithionol
(Synonyms: 硫双二氯酚) 目录号 : GC15976An anthelmintic drug
Cas No.:97-18-7
Sample solution is provided at 25 µL, 10mM.
IC50: 19 μM – 60 μM for various ovarian cancer cell lines
Bithionol is a potent inhibitor of soluble adenylyl cyclase (sAC).
Adenylyl cyclase is an enzyme with critical regulatory roles in cells. All classes of adenylyl cyclases can catalyse the conversion of adenosine triphosphate to 3',5'-cyclic AMP and pyrophosphate.
In vitro: Bithionol could cause dose-dependent cytotoxicity toward all tested ovarian cancer cell lines regardless of their sensitivities to cisplatin. Moreover, such cell death appeared to be via caspases mediated apoptosis. In addition, the mechanism of action appeared to be partially by cell cycle arrest, ROS generation as well as ATX inhibition [1].
In vivo: Oral toxicity of bithionol sulfoxide was assessed in acute toxicity studies in mice and rats. The median lethal dose (LD50) values in mice were > 1000 mg/kg and < 5000 mg/kg after 21 days; the male rat LD50 value was around 5000 mg/kg after 48 h. Moreover, the hepatic toxicity was observed at all tested doses. Increases in serum AST were observed with the high doses, suggesting that mitochondria were affected. In addition, the histological study indicated more intense periportal fatty infiltration with high doses at 5000 and 500 mg/kg [2].
Clinical trial: In a previous study, bithionol was orally given to patients with acute fascioliasis at the daily dose of 25 mg/kg for 10 days. Results showed that all patients were cured. The follow-up period after the first course of treatment was between 16 and 47 months and no major side effects were found [3].
References:
[1] Ayyagari VN,Brard L. Bithionol inhibits ovarian cancer cell growth in vitro - studies on mechanism(s) of action. BMC Cancer.2014 Feb 4;14:61.
[2] Lavric A, Skubic V, Senk L, Lukanc G, Kacl E. Oral toxicity of bithionol sulfoxide in mice and rats. Zbornik Veterinarske Fakultete Univerza Ljubljana 1990 27(1): 33-39
[3] Bacq Y,Besnier JM,Duong TH,Pavie G,Metman EH,Choutet P. Successful treatment of acute fascioliasis with bithionol. Hepatology.1991 Dec;14(6):1066-9.
Cas No. | 97-18-7 | SDF | |
别名 | 硫双二氯酚 | ||
化学名 | 6,6'-thiobis(2,4-dichlorophenol) | ||
Canonical SMILES | ClC1=CC(Cl)=C(O)C(SC2=CC(Cl)=CC(Cl)=C2O)=C1 | ||
分子式 | C12H6Cl4O2S | 分子量 | 356.05 |
溶解度 | DMSO: 20mg/mL | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.8086 mL | 14.043 mL | 28.0859 mL |
5 mM | 0.5617 mL | 2.8086 mL | 5.6172 mL |
10 mM | 0.2809 mL | 1.4043 mL | 2.8086 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.00%
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