MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 329880 | Name: Thioridazine HCl
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Thioridazine is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. The branded product was withdrawn worldwide in 2005 because it caused severe cardiac arrhythmias. However, generic versions are still available in the US.

Chemical Structure

Thioridazine HCl
Thioridazine HCl
CAS#130-61-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 329880

Name: Thioridazine HCl

CAS#: 130-61-0 (HCl)

Chemical Formula: C21H27ClN2S2

Exact Mass: 0.0000

Molecular Weight: 407.03

Elemental Analysis: C, 61.97; H, 6.69; Cl, 8.71; N, 6.88; S, 15.75

Price and Availability

Size Price Availability Quantity
1g USD 150.00 Ready to ship
2g USD 250.00 Ready to ship
5g USD 350.00 2 Weeks
10g USD 450.00 2 weeks
25g USD 750.00 2 weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
130-61-0 (HCl) 50-52-2 (free base)
Synonym
Thioridazine HCl, Aldazine; Mellaril; Melleril; Melzine; NSC 186060; USAF SZ-3; USAF SZ-B; Sonapax hydrochloride; Thioridazine chloride;
IUPAC/Chemical Name
10-[2-(1-methyl-2-piperidinyl)ethyl]-2-(methylthio)-10H-phenothiazine, hydrochloride
InChi Key
NZFNXWQNBYZDAQ-UHFFFAOYSA-N
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
SMILES Code
CSC(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Thioridazine was voluntarily discontinued by its manufacturer, Novartis, worldwide because it caused severe cardiac arrhythmias. Its primary use in medicine was the treatment of schizophrenia. It was also tried with some success as a treatment for various psychiatric symptoms seen in people with dementia, but chronic use of thioridazine and other anti-psychotics in people with dementia is not recommended.
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#C9M01C02
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
Thioridazine hydrochloride is an antipsychotic drug, used in the treatment of schizophrenia and psychosis, shows D4 selectivity or serotonin antagonism.
In vitro activity:
To investigate whether thioridazine inhibited the proliferation of melanoma cells, B16-F10 murine tumor cells were exposed to various concentrations of thioridazine, and then MTT assay was performed. It was observed that after exposure to thioridazine, the absorbance at OD570 nm was reduced in a dose dependent manner (Fig. 1). To compare the anti-proliferation effect of thioridazine with cisplatin, which was commonly used chemotherapeutic agent in patients with melanoma, B16-F10 tumor cells were also exposed to various dose of cisplatin. It was found that high dose of thioridazine showed a more potent and rapid anti-proliferative effect than cisplatin. Collectively, those data suggest that psychotropic agent thioridazine has a suppressive effect on melanoma cells’ multiplication. Unexpectedly, after thioridazine treatment for 24 h, B16-F10 melanoma cells showed more vacuoles in the cytoplasm (Fig. 2A). To investigate whether those cells underwent endoplamic reticulum stress, the cells were subjected to immunoblotting for BiP and CHOP, two markers of ER stress. However, determination of those two molecules showed no remarkable alteration of protein level due to thioridazine treatment (Fig. 2B). Autophagy markers were then assessed. As shown in Fig. 2, tumor lysates were then immunoblotted for LC3. Interestingly, there were more LC3II after thioridazine treatment compared to unexposed samples (Fig. 2C), suggestive of autophagy induction. To summarize, thioridazine could induce autophagy in melanoma cells. Reference: Biomed Pharmacother. 2018 Jan;97:833-837. https://linkinghub.elsevier.com/retrieve/pii/S0753-3322(17)32578-7
In vivo activity:
The immune cells in the tumor microenvironment were analyzed after thioridazine therapy. Thioridazine did not significantly change the proportion of CD11b + F4/80 + CD206+ M2 macrophagaes. Though it slightly increased the NK cells percent, but it did not reach statistical significance (Fig. 5A). The microvessel density was evaluated in the tumor microevironment after thioridazine therapy. As seen in Fig. 5B–C, it was found that thioridazine remarkably reduced the tumor vasculature. Collectively, these data indicated that thioridazine exhibited in vivo anti-tumor effect in syngeneic melanoma model. Reference: Biomed Pharmacother. 2018 Jan;97:833-837. https://linkinghub.elsevier.com/retrieve/pii/S0753-3322(17)32578-7
Solvent mg/mL mM comments
Solubility
DMSO 81.0 198.99
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 407.03 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
1. Jiang X, Chen Z, Shen G, Jiang Y, Wu L, Li X, Wang G, Yin T. Psychotropic agent thioridazine elicits potent in vitro and in vivo anti-melanoma effects. Biomed Pharmacother. 2018 Jan;97:833-837. doi: 10.1016/j.biopha.2017.11.012. Epub 2017 Nov 6. PMID: 29136758. 2. Christensen JB, Hendricks O, Chaki S, Mukherjee S, Das A, Pal TK, Dastidar SG, Kristiansen JE. A comparative analysis of in vitro and in vivo efficacies of the enantiomers of thioridazine and its racemate. PLoS One. 2013;8(3):e57493. doi: 10.1371/journal.pone.0057493. Epub 2013 Mar 7. PMID: 23505431; PMCID: PMC3591432.
In vivo protocol:
1. Jiang X, Chen Z, Shen G, Jiang Y, Wu L, Li X, Wang G, Yin T. Psychotropic agent thioridazine elicits potent in vitro and in vivo anti-melanoma effects. Biomed Pharmacother. 2018 Jan;97:833-837. doi: 10.1016/j.biopha.2017.11.012. Epub 2017 Nov 6. PMID: 29136758. 2. Christensen JB, Hendricks O, Chaki S, Mukherjee S, Das A, Pal TK, Dastidar SG, Kristiansen JE. A comparative analysis of in vitro and in vivo efficacies of the enantiomers of thioridazine and its racemate. PLoS One. 2013;8(3):e57493. doi: 10.1371/journal.pone.0057493. Epub 2013 Mar 7. PMID: 23505431; PMCID: PMC3591432.