甲醚硫酮可提高谷胱甘肽水平和 II 相解毒酶，是一种利胆剂（一种刺激胆汁生成的药物），也是保护肝脏的 H2S 缓释供体。通过加快肝脏和结肠中致癌物质的解毒速度，茴香三硫酮是一种潜在有用的肺癌化学预防药物，对其他靶器官也具有化学预防作用。脑缺血后，茴香脑三硫酮可以保护血脑屏障的完整性[2]。

当长期用茴香三硫酮治疗时，通过电刺激副交感神经元和注射毛果芸香碱，可以增加大鼠颌下腺唾液的产生。毒蕈碱乙酰胆碱受体随着唾液分泌的增加而增加[3]。

Absorption, Distribution and Excretion
While anethole trithione (ATT) exhibits high lipophilicity (log P = 3.8) and high intestinal permeability, its water solubility is extremely low (0.38 ug/ml). This low solubility limits the solubility and bioavailability of ATT. Nevertheless, in 22 healthy Chinese volunteers, after administration of ATT, the observed Cmax was approximately 0.98 ± 0.49 ng/mL, and the recorded Tmax was 2.2 ± 1.9 h. Although this drug has been studied and discussed since the 1980s, detailed pharmacokinetic information has not been readily available, and limited new pharmacokinetic data were only recently established (in 2007). However, the low absorption and bioavailability of anethole trithione indicate that any type of volume of distribution measurement may not be entirely accurate. Although this drug has been studied and discussed since the 1980s, detailed pharmacokinetic information has not been readily available, and limited new pharmacokinetic data were only recently (2007). Nevertheless, the estimated clearance of anethole trithione observed after oral administration of an aqueous suspension to rats was approximately 113.20 ± 52.37 L/h/kg. Metabolites/Metabolites Anethole trithione (ATT) is rapidly metabolized to 4-hydroxyanisole trithione via O-demethylation. This metabolite exhibits pharmacological activity similar to its parent, ATT. Some studies have proposed that this metabolism occurs in hepatic microsomes, but this hypothesis and the specific hepatic cytochrome P450 isoenzymes involved in this metabolism have not been formally elucidated.

---

Biological Half-Life
Although this drug was studied and discussed as early as the 1980s, detailed pharmacokinetic information was not readily available, and limited new pharmacokinetic data were only recently (2007). Therefore, after administration of anethole trithione to 22 healthy Chinese volunteers, the observed half-life was approximately 3.78 ± 2.12 hours.

Protein Binding

Although the drug was studied and discussed as early as the 1980s, detailed pharmacokinetic information about it was not readily available, and limited new pharmacokinetic data for the drug were only recently determined (most recently in 2007).

[1]. Enhancement of salivary secretion and neuropeptide (substance P, alpha-calcitonin gene-related peptide) levels in saliva by chronic anethole trithione treatment. J Pharm Pharmacol. 2001 Dec;53(12):1697-702.

[2]. Synthesis, Characterization, and In Vivo Evaluation of Desmethyl Anethole Trithione Phosphate Prodrug for Ameliorating Cerebral Ischemia-Reperfusion Injury in Rats. ACS Omega. 2020 Feb 24;5(9):4595-4602.

[3]. Chronic anethole trithione treatment enhances the salivary secretion and increases the muscarinic acetylcholine receptors in the rat submaxillary gland. Arch Int Pharmacodyn Ther. 1984 Oct;271(2):206-12.

Pharmacodynamics
Anethole trithione (ATT) exhibits high lipophilicity (log P = 3.8) but extremely low water solubility (0.38 μg/mL), limiting its dissolution and absorption. Furthermore, ATT is rapidly metabolized to 4-hydroxyanisole trithione (ATX, with similar pharmacological activity to ATT) via O-demethylation. Therefore, ATT plasma concentrations are typically low, resulting in limited oral bioavailability. Given these pharmacodynamic characteristics, researchers continue to focus on developing carriers that can improve the in vivo bioavailability of ATT.

C10H8OS3

240.35

239.973

532-11-6

Anethole;104-46-1

2194

Yellow to orange solid powder

1.4±0.1 g/cm3

398.1±52.0 °C at 760 mmHg

23 C

194.6±30.7 °C

0.0±0.9 mmHg at 25°C

1.732

3.39

105.5

0

4

2

14

254

0

KYLIZBIRMBGUOP-UHFFFAOYSA-N

InChI=1S/C10H8OS3/c1-11-8-4-2-7(3-5-8)9-6-10(12)14-13-9/h2-6H,1H3

5-(4-methoxyphenyl)dithiole-3-thione

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~12.5 mg/mL (~52.01 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (10.40 mM) (饱和度未知) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80+，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。