Thioridazine (Synonyms: 硫利达嗪)

目录号: HY-B0965A 纯度: 99.50%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Thioridazine 是一种具有口服活性的多巴胺受体 D2 家族蛋白的拮抗剂，具有有效的抗焦虑活性。Thioridazine 也是一种有效的 PI3K-Akt-mTOR 信号通路的抑制剂，具有抗血管生成作用。Thioridazine 在多种类型的癌细胞中显示出抗增殖和凋亡诱导作用，对靶向癌症干细胞 (CSCs) 具有特异性。

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Thioridazine Chemical Structure

CAS No. : 50-52-2

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MCE 顾客使用本产品发表的 4 篇科研文献

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

生物活性
纯度 & 产品资料
参考文献

生物活性

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)^[1]^[2]^[3]^[4].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3.5 μM Compound: thioridazine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HBL1	GI₅₀	6.6 μM Compound: Thioridazine	Antiproliferative activity against human HBL1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human HBL1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 34181850]
HEK293	IC₅₀	1.32 μM Compound: Thioridazine	Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit	[PMID: 22761000]
HEK293	IC₅₀	1830 nM Compound: Thioridazine	Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA	[PMID: 21300721]
J774	IC₅₀	4.1 μg/mL Compound: 1; TZ	Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay	[PMID: 28039773]
KG-1a	IC₅₀	6.01 μM Compound: THD	Antiproliferative activity against human KG1a cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human KG1a cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 31541872]
L5178Y	IC₅₀	12.72 nM Compound: TZ	Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay	[PMID: 32871268]
L5178Y	IC₅₀	12.72 μM Compound: TZ	Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27156771]
L5178Y	IC₅₀	7.43 nM Compound: TZ	Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay	[PMID: 32871268]
L5178Y	IC₅₀	7.43 μM Compound: TZ	Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 27156771]
Macrophage cell line	CC₅₀	13.8 μM Compound: TZ	Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay	[PMID: 28964936]
MCF7	IC₅₀	12.95 μM Compound: THD	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 31541872]
MDA-MB-231	IC₅₀	14.19 μM Compound: THD	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 31541872]
MRC5	IC₅₀	8.2 μg/mL Compound: 1; TZ	Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay	[PMID: 28039773]
OCI-Ly1	GI₅₀	13.4 μM Compound: Thioridazine	Antiproliferative activity against human OCI-Ly1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human OCI-Ly1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 34181850]
PBMC	IC₅₀	13.78 μM Compound: TZ	Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay	[PMID: 26197353]
SK-BR-3	IC₅₀	18.23 μM Compound: THD	Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 31541872]
SUM-159-PT	IC₅₀	14.51 μM Compound: THD	Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability incubated for 2 days by MTT assay Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability incubated for 2 days by MTT assay	[PMID: 31541872]
TMD8	GI₅₀	5.9 μM Compound: Thioridazine	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay	[PMID: 34181850]
Ventricular myocyte	IC₅₀	1.3 μM Compound: Thioridazine	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Ventricular myocyte	IC₅₀	1300 nM Compound: Thioridazine	Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes	[PMID: 21300721]
Vero	CC₅₀	15.96 μM Compound: Thioridazine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	17.79 μg/mL Compound: Tz	Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay	[PMID: 32526553]
Vero	IC₅₀	5.3 μg/mL Compound: thioridazine	Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay	[PMID: 25238443]
Vero	IC₅₀	6.69 μM Compound: Thioridazine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

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^[2].
Thioridazine (15 μM; 24 h) reduces cell viability of the cervical (HeLa, Caski and C33A) and endometrial (HEC-1-A and KLE) cancer cells^[4].
Thioridazine (1-15 μM; 24-48 h) induces gastric cancer cell death via the mitochondrial apoptosis pathway and mitochondrial pathway^[2].
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 ^[4].
Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains of A. baumannii^[3].

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

Cell Viability Assay^[1]

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^[1]

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^[5].
Thioridazine (1.0-5.0 mg/kg; s.c.) reduces oral behavior and selectively blocks repetitive head bobbing^[1].

MCE 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^[5]
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.

Clinical Trial

分子量

370.57

Formula

C₂₁H₂₆N₂S₂

CAS 号

50-52-2

性状

油状物

颜色

Colorless to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (269.85 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6985 mL	13.4927 mL	26.9855 mL
5 mM	0.5397 mL	2.6985 mL	5.3971 mL
10 mM	0.2699 mL	1.3493 mL	2.6985 mL

查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.50%

选择批次：

Data Sheet (631 KB) SDS (392 KB)

COA (290 KB) HNMR (250 KB) LCMS (86 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Tschanz JT, et, al. Atypical antipsychotic drugs block selective components of amphetamine-induced stereotypy. Pharmacol Biochem Behav. 1988 Nov;31(3):519-22. [Content Brief]

[2]. Mu J, et, al. Thioridazine, an antipsychotic drug, elicits potent antitumor effects in gastric cancer. Oncol Rep. 2014 May;31(5):2107-14. [Content Brief]

[3]. Kang S, et, al. Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells. Apoptosis. 2012 Sep;17(9):989-97. [Content Brief]

[4]. Loehr AR, et, al. Targeting Cancer Stem Cells with Differentiation Agents as an Alternative to Genotoxic Chemotherapy for the Treatment of Malignant Testicular Germ Cell Tumors. Cancers (Basel). 2021 Apr 23;13(9):2045. [Content Brief]

Thioridazine 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6985 mL	13.4927 mL	26.9855 mL	67.4636 mL
	5 mM	0.5397 mL	2.6985 mL	5.3971 mL	13.4927 mL
	10 mM	0.2699 mL	1.3493 mL	2.6985 mL	6.7464 mL
	15 mM	0.1799 mL	0.8995 mL	1.7990 mL	4.4976 mL
	20 mM	0.1349 mL	0.6746 mL	1.3493 mL	3.3732 mL
	25 mM	0.1079 mL	0.5397 mL	1.0794 mL	2.6985 mL
	30 mM	0.0900 mL	0.4498 mL	0.8995 mL	2.2488 mL
	40 mM	0.0675 mL	0.3373 mL	0.6746 mL	1.6866 mL
	50 mM	0.0540 mL	0.2699 mL	0.5397 mL	1.3493 mL
	60 mM	0.0450 mL	0.2249 mL	0.4498 mL	1.1244 mL
	80 mM	0.0337 mL	0.1687 mL	0.3373 mL	0.8433 mL
	100 mM	0.0270 mL	0.1349 mL	0.2699 mL	0.6746 mL

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Thioridazine (Synonyms: 硫利达嗪)

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MCE 顾客使用本产品发表的 4 篇科研文献

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Thioridazine (Synonyms: 硫利达嗪)

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Other Forms of Thioridazine:

Thioridazine 相关抗体

MCE 顾客使用本产品发表的 4 篇科研文献

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