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盐酸硫利达嗪 (Synonyms: 盐酸硫利达嗪)
目录号: PC14877 纯度: ≥98%
CAS No. :130-61-0
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PC14877-100mg 100mg ¥509.60 请登录
PC14877-500mg 500mg ¥744.80 请登录
PC14877-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥539.00 请登录
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中文名称
盐酸硫利达嗪
中文别名
盐酸硫利达嗪;硫利哌啶;甲硫达嗪;盐酸甲硫达嗪;硫利达嗪盐酸盐;甲硫哒嗪盐酸盐;N-Boc-4-[(2-甲基-5-苯并噻唑基)甲基]哌啶;氨基硫脲;特戊酸氟米松;盐酸甲硫哒嗪 EP标准品;盐酸硫利达嗪 USP标准品;盐酸硫利达嗪 标准品;10-[2-(1-甲基-2-哌啶基)乙基]-2-(甲硫基)-10H-吩噻嗪盐酸盐;硫利达嗪,盐酸D3;盐酸硫代利哒;10-[2-(1-甲基哌啶-2-基)乙基]-2-(甲硫基)-10H-吩噻嗪盐酸盐;甲硫达嗪盐酸盐
英文名称
thioridazine hydrochloride
英文别名
thioridazine hydrochloride;THIORIDAZINE HCL;10-[2-(1-METHYL-2-PIPERIDYL)ETHYL]-2-(METHYLTHIO)-10H-PHENOTHIAZINE HYDROCHLORIDE;10-[2-(1-METHYL-2-PIPERIDYL)-ETHYL]-2-[METHYLTHIOL]-PHENOTHIAZINE HYDROCHLORIDE;10-(2-(1-methyl-2-piperidinyl)ethyl)-2-(methylthio)-10h-phenothiazinmono;10H-Phenothiazine, 10-[2-(1-methyl-2-piperidinyl)ethyl]-2-(methylthio)-, monohydrochloride (9CI);Novoridazine;Thioridazine;Thioridazine (hydrochloride);Thioridazine Hydroch;10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfanylphenothiazine,hydrochloride;Mellaril;10-[2-(1-Methylpiperidin-2-yl)ethyl]-2-(methylthio)-10H-phenothiazine Hydrochloride;Phenothiazine, 10-[2-(1-methyl-2-piperidyl)ethyl]-2-(methylthio)-,hydrochloride (6CI,7CI);Phenothiazine,10-[2-(1-methyl-2-piperidyl)ethyl]-2-(methylthio)-, monohydrochloride (8CI);10-[3-(1-Methyl-2-piperidyl)ethyl]-2-(methylthio)phenothiazine hydrochloride;2-Methylmercapto-10-[2-(N-methyl-2-piperidyl)ethyl]phenothiazine hydrochloride;Aldazine;Mallorol;Mellaril hydrochloride;Melleretten;Melleril;Melleril (tablet);NSC 186060;Orsanil;Ridazin;Stalleril;10H-Phenothiazine,10-[2-(1-methyl-2-piperidinyl)ethyl]-2-(methylthio)-, hydrochloride (1:1);usafsz-3;USAF SZ-B;ThioridazinHCl;10H-Phenothiazine,10-[2-(1-methyl-2-piperidinyl)ethyl]-2-(methylthio)-, monohydrochloride (9CI);melleril(tablet)
Cas No.
130-61-0
分子式
C21H26N2S2.HCl
分子量
407.03
包装储存

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

性状

Solid

IC50 & Target[1][2]

serotonin

 

体外研究(In Vitro)

Thioridazine (0.01-100 μM; 48 h) reduces the cell viability of NCI-N87 and AGS cells in a concentration-dependent manner.
Thioridazine (15 μM; 24 h) reduces cell viability of the cervical (HeLa, Caski and C33A) and endometrial (HEC-1-A and KLE) cancer cells.
Thioridazine (1-15 μM; 24-48 h) induces gastric cancer cell death via the mitochondrial apoptosis pathway and mitochondrial pathway.
Thioridazine (15 μM; 24 h) modulates the regulation of cell cycle progression by interfering with the PI3K/Akt pathway and induces G1 cell cycle arrest in cervical and endometrial cancer cells .
Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains of A. baumannii.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: NCI-N87 and AGS cells
Concentration: 0.01, 0.1, 0.5, 1, 5, 10, 20, 50, 100 μM
Incubation Time: 48 hours
Result: Exhibited cytotoxicity in gastric cancer cells.

Western Blot Analysis

Cell Line: NCI-N87 and AGS cells
Concentration: 1, 5, 10, 15 μM
Incubation Time: 24, 48 hours
Result: Downregulated the precursors of caspase-9, caspase-8 and caspase-3.
体内研究(In Vivo)

Thioridazine (25 mg/kg; i.p. every 3 days for 3 weeks) extends the survival of tumor-bearing mice and reduces the number of pluripotent embryonal carcinoma (EC) cells within tumors.
Thioridazine (1.0-5.0 mg/kg; s.c.) reduces oral behavior and selectively blocks repetitive head bobbing.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude and Rag2KO mice were injected with iPS cells or NT2D1 cells
Dosage: 25 mg/kg
Administration: I.p. every 3 days for 3 weeks
Result: Reduced the number of OCT4-expressing cells within malignant teratocarcinomas and extended the survival of tumor-bearing mice.
With no effect on fertility.
运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

H2O : 100 mg/mL (245.68 mM; Need ultrasonic)

DMSO : ≥ 45 mg/mL (110.55 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4568 mL 12.2838 mL 24.5676 mL
5 mM 0.4914 mL 2.4568 mL 4.9135 mL
10 mM 0.2457 mL 1.2284 mL 2.4568 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 12.5 mg/mL (30.71 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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