| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| 25g |
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Purity: ≥98%
Chlorprothixene HCl is a typical antipsychotic drug of the thioxanthene class and an antagonist of dopamine and histamine receptors such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively. It was the series' first synthesized product. Chlorprothixene has little affinity for H3, but it exhibits strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, and H1, with Ki values of 18 nM, 2.96 nM, 4.56 nM, 9 nM, and 3.75 nM, respectively. Furthermore, rat 5-HT6 from stably transfected HEK-293 cells and rat 5-HT7 receptors from transiently expressed COS-7 cells exhibit strong affinities for chlorprothixene, with Ki values of 3 nM and 5.6 nM, respectively.
| Targets |
Human D1 Receptor ( Ki = 18 nM ); Human D2 Receptor ( Ki = 2.96 nM ); Human D3 Receptor ( Ki = 4.56 nM ); Human D5 Receptor ( Ki = 9 nM ); Human H1 Receptor ( Ki = 3.75 nM )
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| ln Vitro |
Chlorprothixene adsorbs and binds to 5-HT, and its pKi for 5-HT7, 5-HT6 and 5-HT2 are 8.3, 8.5 and 9.4 respectively [2].
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| References |
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| Molecular Formula |
C18H19CL2NS
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|---|---|
| Molecular Weight |
352.32116
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| Exact Mass |
351.06
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| Elemental Analysis |
C, 61.36; H, 5.44; Cl, 20.12; N, 3.98; S, 9.10
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| CAS # |
6469-93-8
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| Related CAS # |
Chlorprothixene; 113-59-7; Chlorprothixene-d6 hydrochloride
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| Appearance |
Solid powder
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| SMILES |
CN(C)CC/C=C\1/C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl
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| InChi Key |
YWKRLOSRDGPEJR-KIUKIJHYSA-N
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| InChi Code |
InChI=1S/C18H18ClNS.ClH/c1-20(2)11-5-7-14-15-6-3-4-8-17(15)21-18-10-9-13(19)12-16(14)18;/h3-4,6-10,12H,5,11H2,1-2H3;1H/b14-7-;
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| Chemical Name |
(3Z)-3-(2-chlorothioxanthen-9-ylidene)-N,N-dimethylpropan-1-amine;hydrochloride
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| Synonyms |
Truxal; Taractan; Minithixen; Truxal hydrochloride; Chlorprothixene; NSC 169899; NSC 56379; NSC 78193
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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) |
H2O: ~25 mg/mL (~71 mM)
Ethanol: ~25 mg/mL (~71 mM) DMSO: 2.5~70 mg/mL (7.1~198.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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: ≥ 2.5 mg/mL (7.10 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8383 mL | 14.1916 mL | 28.3833 mL | |
| 5 mM | 0.5677 mL | 2.8383 mL | 5.6767 mL | |
| 10 mM | 0.2838 mL | 1.4192 mL | 2.8383 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03449485 | Recruiting | Drug: Chlorprothixene | Obesity, Morbid | Norwegian University of Science and Technology |
January 2, 2018 | N/A |
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