| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Thioridazine HCl primarily targets the dopamine D2 receptor in the mesolimbic system, decreasing dopamine activity to alleviate psychotic symptoms such as hallucinations and delusions. It also binds to serotonin 5-HT2 receptors, decreasing serotonin activity. It acts as a calcium channel blocker and has been shown to target the PI3-K/Akt/mTOR/p70 S6K pathway to induce apoptosis and G1 cell cycle arrest in cancer cells.
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| 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].
Thioridazine HCl exhibits antiproliferative and apoptosis-inducing effects in various cancer cell lines, including cervical, endometrial, and breast cancer cells. It triggers apoptosis by targeting the PI3-K/Akt/mTOR/p70 S6K pathway and induces G1 cell cycle arrest. It also displays antibacterial activity. It acts as a dopamine D2 receptor antagonist and calcium channel blocker. |
| 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].
Thioridazine HCl has been shown to successfully kill human cancer stem cells (CSCs). Its in vivo effects are primarily related to its antipsychotic activity, reducing psychotic symptoms in patients with schizophrenia. It exhibits sedative and anti-anxiety activities. Its antibacterial and anticancer properties are being investigated in preclinical models. |
| Enzyme Assay |
In vitro receptor binding assays for Thioridazine HCl measure its affinity for dopamine D2 and serotonin 5-HT2 receptors. The compound is incubated with membrane preparations expressing the receptors and a radiolabeled ligand, and displacement is measured. Calcium channel blocking activity can be assessed using patch-clamp electrophysiology. Kinase inhibition assays can evaluate its effects on the PI3-K/Akt/mTOR pathway.
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| 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. In vitro cellular assays for Thioridazine HCl are used to assess its anticancer and antibacterial activities. Cancer cell lines are treated with the compound, and cell viability is measured using MTT or similar assays. Apoptosis is detected by flow cytometry using Annexin V staining. Cell cycle analysis is performed using propidium iodide staining. Antibacterial activity is assessed using broth microdilution or agar diffusion methods. |
| 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. In vivo animal models for Thioridazine HCl are primarily used to study its antipsychotic effects. Rodent models of schizophrenia, such as the amphetamine-induced hyperactivity model or the prepulse inhibition test, are used to evaluate its efficacy. Its anticancer activity can be studied in xenograft mouse models, where tumor growth is measured after treatment with the compound. |
| ADME/Pharmacokinetics |
Thioridazine HCl is well-absorbed after oral administration and is extensively metabolized in the liver. It is highly protein-bound and has a long half-life. Its metabolism involves hepatic cytochrome P450 enzymes, particularly CYP2D6. The compound and its metabolites are excreted in urine and feces. Its pharmacokinetics can be affected by genetic polymorphisms in CYP2D6, leading to variability in drug levels and response.
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| Toxicity/Toxicokinetics |
Thioridazine HCl is associated with a significant risk of cardiac toxicity, including QT interval prolongation and torsades de pointes, which has limited its clinical use. Other side effects include extrapyramidal symptoms, sedation, weight gain, and anticholinergic effects. Due to its cardiotoxicity, thioridazine is now rarely used as a first-line antipsychotic and is reserved for patients who have not responded to other treatments.
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| References |
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| Additional Infomation |
Thioridazine hydrochloride is a hydrochloride salt. It is a first-generation antipsychotic and anti-aging drug. It contains a thioridazine group. Thioridazine hydrochloride is the hydrochloride form of thioridazine, a piperidine phenothiazine derivative and a dopamine antagonist with antipsychotic effects. Thioridazine hydrochloride binds to the postsynaptic dopamine receptor D2 in the mesolimbic system, thereby reducing dopamine activity and alleviating psychotic symptoms such as hallucinations and delusions. In addition, the drug also binds to serotonin 2 receptors, leading to a decrease in serotonin activity. A phenothiazine antipsychotic drug used to treat mental illnesses, including schizophrenia. See also: Thioridazine (containing the active moiety).
Thioridazine HCl is a phenothiazine antipsychotic with dopamine D2 receptor antagonist activity. It has been used to treat schizophrenia and other psychotic disorders. It also exhibits antibacterial, anti-angiogenic, and anticancer properties, including the ability to kill cancer stem cells. It induces apoptosis via the PI3-K/Akt/mTOR/p70 S6K pathway and causes G1 cell cycle arrest. |
| Molecular Formula |
C21H26N2S2.HCL
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|---|---|
| Molecular Weight |
407.03
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| Exact Mass |
406.13
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| CAS # |
130-61-0
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| Related CAS # |
Thioridazine;50-52-2
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| PubChem CID |
66062
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| Appearance |
White to off-white solid powder
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| Boiling Point |
515.7ºC at 760 mmHg
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| Melting Point |
158-1600C
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| Flash Point |
265.7ºC
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| Vapour Pressure |
9.65E-11mmHg at 25°C
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| LogP |
6.69
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
432
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NZFNXWQNBYZDAQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26N2S2.ClH/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23;/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1H
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| Chemical Name |
10-[2-(1-methylpiperidin-2-yl)ethyl]-2-methylsulfanylphenothiazine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~245.68 mM)
DMSO : ≥ 45 mg/mL (~110.55 mM) |
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| 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. View More
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. 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). |
| 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.
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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