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Thioridazine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thioridazine hydrochloride图片
CAS NO:130-61-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
盐酸硫利达嗪;盐酸硫代利哒;甲硫达嗪盐酸盐;甲硫哒嗪盐酸盐
产品介绍
Thioridazine hydrochloride 是一种具有口服活性的多巴胺受体D2家族蛋白的拮抗剂,具有有效的的抗焦虑活性。Thioridazine hydrochloride 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 hydrochloride 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。
生物活性

Thioridazine hydrochloride, an orally active antagonist of thedopamine receptorD2family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor ofPI3K-Akt-mTORsignaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative andapoptosisinduction effects in various types ofcancercells, with specificity on targetingcancer stem cells(CSCs)[1][2][3][4].

IC50& Target

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[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 G1cell cycle arrest in cervical and endometrial cancer cells[4].
Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains ofA. baumannii[3].

Cell Proliferation 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].

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

407.04

性状

Solid

Formula

C21H27ClN2S2

CAS 号

130-61-0

中文名称

盐酸硫利达嗪;盐酸硫代利哒;甲硫达嗪盐酸盐;甲硫哒嗪盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据
In Vitro: 

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

DMSO : ≥ 45 mg/mL(110.55 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4568 mL12.2838 mL24.5676 mL
5 mM0.4914 mL2.4568 mL4.9135 mL
10 mM0.2457 mL1.2284 mL2.4568 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: PBS

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

  • 2.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在本网站选购。