Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Mesoridazine is a potent phenothiazine dopamine receptor anatagonist that is able to inhibit D2DR and D4DR. It has a high affinity for dopamine D4 receptor. Mesoridazine besylate is an antipsychotic agent.
ln Vitro |
Mesoridazine inhibits human ether-a-go-go related gene (HERG) currents in a concentration-dependent manner (IC50 = 550 nM, 0 mV). The blocking action increases dramatically along the voltage range where HERG activation occurs, leading to maximal Saturable channel activity when HERG voltage is reached [1]. The total absorption rates of 15.94 ± 4.04% and 39.24 ± 5.11% of mesoridazine (15 mM; 24 hours) in nude mouse and pig skin, respectively, were reported [3].
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ln Vivo |
Mesoridazine (15 mM) shows strong action and persistent analgesia in preventing cutaneous discomfort when applied topically once or once a day for seven days [3]. Mice in the nude were given a topical application of mesoridazine (15 mM) for six hours. The intradermal concentration of the drug was 0.34 - 0.74 nmol/mg [3].
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Animal Protocol |
Animal/Disease Models: 8weeks old female nude mice [3]
Doses: 15 mM Route of Administration: Topical administration, once (analgesic test) or one time/day for 7 days (stimulation test) Experimental Results:Shows analgesic effect. A slight increase in transepidermal water loss (TEWL) from 7.8 to 9.9 g/m2/h was observed. |
References |
[1]. Zhi Su, et al. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60.
[2]. I S M Salih, et al. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54. [3]. Liu KS, et al. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68. |
Molecular Formula |
C21H26N2OS2
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Molecular Weight |
386.57394
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CAS # |
5588-33-0
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Related CAS # |
Mesoridazine benzenesulfonate;32672-69-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=S(C(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4)C
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InChi Key |
SLVMESMUVMCQIY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H26N2OS2/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(26(2)24)15-19(21)23/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3
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Chemical Name |
10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylsulfinyl)-10H-phenothiazine
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Synonyms |
NC-123 NSC 186066 NSC-186066 NSC186066 TPS23 TPS 23 TPS-23 Thioridazine thiomethyl sulfoxide
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5869 mL | 12.9343 mL | 25.8685 mL | |
5 mM | 0.5174 mL | 2.5869 mL | 5.1737 mL | |
10 mM | 0.2587 mL | 1.2934 mL | 2.5869 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.