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Thioridazine HCl

Cat No.:V16339 Purity: ≥98%
Thioridazine HCl is an orally bioactive dopamine receptor D2 family protein antagonist (inhibitor) with potent anxiolytic (anti-anxiety) activity.
Thioridazine HCl
Thioridazine HCl Chemical Structure CAS No.: 130-61-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
500mg
Other Sizes

Other Forms of Thioridazine HCl:

  • Thioridazine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Thioridazine HCl is an orally bioactive dopamine receptor D2 family protein antagonist (inhibitor) with potent anxiolytic (anti-anxiety) activity. Thioridazine HCl is also a potent inhibitor of the PI3K-Akt-mTOR signaling pathway and has anti-angiogenic effects. Thioridazine HCl displays anti-proliferation and apoptosis-inducing effects in multiple types of cancer/tumor cells, with specificity for targeting cancer stem cells (CSCs).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Concentrated thioridazine (0.01-100 μM; 48 h) treatment decreases NCI-N87 and AGS cell viability [2]. Thioridazine (1-15 μM; 24-48 h) promotes cell death via the mitochondrial pathway and pharyngeal pathways. Thioridazine (15 μM; 24 h) lowers cervical (HeLa, Caski, and C33A) and endometrial [2]. Cancer cell viability (HEC-1-A and KLE) [4]. ;24 h) By interfering with PI3K/Akt, it causes cervical cancer cells to develop in the G1 cell cycle [4]. Development of conjugated Bowman immotile cell lines that are susceptible to thioridazine inhibitors [3].
ln Vivo
Thioridazine (25 mg/kg; intraperitoneal injection every three days for three weeks) can decrease the amount of pluripotent cell carcinoma (EC) cells within the tumor and increase the survival time of tumor-bearing animals [5].
Cell Assay
Cell Proliferation Assay[1]
Cell Types: NCI-N87 and AGS Cell
Tested Concentrations: 0.01, 0.1, 0.5, 1, 5, 10, 20, 50, 100 μM
Incubation Duration: 48 hrs (hours)
Experimental Results: demonstrated cytotoxicity in gastric cancer cells .

Western Blot Analysis [1]
Cell Types: NCI-N87 and AGS cells
Tested Concentrations: 1, 5, 10, 15 μM
Incubation Duration: 24, 48 hrs (hours)
Experimental Results: Downregulation of caspase-9, caspase-8 and caspase-3 precursors.
Animal Protocol
Animal/Disease Models: Nude mice and Rag2KO mice were injected with iPS cells or NT2D1 cells [5]
Doses: 25 mg/kg Administration
Doses: 5.0 mg/kg; subcutaneous injection) to reduce oral behavior and selectively prevent repetitive head bobbing [1].
Route of Administration: intraperitoneal (ip) injection every 3 days for 3 weeks.
Experimental Results: diminished the number of OCT4-expressing cells in malignant teratocarcinoma and prolonged the survival of tumor-bearing mice. Has no effect on fertility.
References
[1]. Tschanz JT, et, al. Atypical antipsychotic drugs block selective components of amphetamine-induced stereotypy. Pharmacol Biochem Behav. 1988 Nov;31(3):519-22.
[2]. Mu J, et, al. Thioridazine, an antipsychotic drug, elicits potent antitumor effects in gastric cancer. Oncol Rep. 2014 May;31(5):2107-14.
[3]. Aguilar-Vega L, et, al. Antibacterial properties of phenothiazine derivatives against multidrug-resistant Acinetobacter baumannii strains. J Appl Microbiol. 2021 Apr 22.
[4]. 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.
[5]. 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H26N2S2.HCL
Molecular Weight
407.03
CAS #
130-61-0
Related CAS #
Thioridazine;50-52-2
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
CSC(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4.[H]Cl
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~245.68 mM)
DMSO : ≥ 45 mg/mL (~110.55 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 12.5 mg/mL (30.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4568 mL 12.2841 mL 24.5682 mL
5 mM 0.4914 mL 2.4568 mL 4.9136 mL
10 mM 0.2457 mL 1.2284 mL 2.4568 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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