Size | Price | Stock | Qty |
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500mg |
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1g |
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5g |
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10g |
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25g |
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Other Sizes |
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Purity: ≥98%
Chlorpromazine HCl (Promacid; Chloractil; Klorpromex; Fenactil; Largactil; Propaphenin; Sonazine; Thorazine), the Hydrochloride salt form of chlorpromazine, is a potent dopamine and potassium channel inhibitor used as an antipsychotic medication for the treatment of psychotic disorders such as schizophrenia. It blocks the dopamine and potassium channels, exhibiting IC50 values of 6.1 and 16 μM for time-independent outward currents and inward-rectifying K+ currents, respectively. A classic antipsychotic drug with phenothiazine properties and anti-emetic properties is chlorpromazine hydrochloride (HCl). It prevents the brain from having too much dopamine by blocking postsynaptic dopamine receptors in limbic and cortical regions. This has an antipsychotic effect.
Targets |
D2 dopamine receptors (Ki = 363 nM ); 5-HT2A (Ki = 8.3 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Recent studies have emphasized that nonequilibrium conditions of postsynaptic GABAA receptor (GABAAR) activation is a key factor in shaping the time course of IPSCs (Puia et al., 1994; Jones and Westbrook, 1995). Such nonequilibrium, resulting from extremely fast agonist time course, may affect the interaction between pharmacological agents and postsynaptic GABAARs. In the present study we found that chlorpromazine (CPZ), a widely used antipsychotic drug known to interfere with several ligand and voltage-gated channels, reduces the amplitude and accelerates the decay of miniature IPSCs (mIPSCs). A good qualitative reproduction of the effects of CPZ on mIPSCs was obtained when mIPSCs were mimicked by responses to ultrafast GABA applications to excised patches. Our experimental data and model simulations indicate that CPZ affects mIPSCs by decreasing the binding (kon) and by increasing the unbinding (koff) rates of GABAARs. Because of reduction of kon by CPZ, the binding reaction becomes rate-limiting, and agonist exposure of GABAARs during mIPSC is too short to activate the receptors to the same extent as in control conditions. The increase in unbinding rate is implicated as the mechanism underlying the acceleration of mIPSC decaying phase. The effect of CPZ on GABAAR binding rate, resulting in slower onset of GABA-evoked currents, provides a tool to estimate the speed of synaptic clearance of GABA. Moreover, the onset kinetics of recorded responses allowed the estimate the peak synaptic GABA concentration [1].
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Cell Assay |
Cell Line: U-87MG glioma cells
Concentration: 0, 10, 20, 40 μM Incubation Time: 0, 24, 48 h Result: Showed anti-proliferative activity in a dose- and time-dependent manner. |
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Animal Protocol |
5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2]
20 mg/kg Injected intraperitoneally; single daily for 7 days |
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References |
Molecular Formula |
C17H20CL2N2S
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Molecular Weight |
355.33
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Exact Mass |
354.07
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Elemental Analysis |
C, 57.46; H, 5.67; Cl, 19.96; N, 7.88; S, 9.02
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CAS # |
69-09-0
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Related CAS # |
Chlorpromazine; 50-53-3; Chlorpromazine-d6 hydrochloride; 1228182-46-4
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Appearance |
White to off-white crystalline powder
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LogP |
5.76
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tPSA |
31.78
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SMILES |
CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl
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InChi Key |
FBSMERQALIEGJT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H19ClN2S.ClH/c1-19(2)10-5-11-20-14-6-3-4-7-16(14)21-17-9-8-13(18)12-15(17)20;/h3-4,6-9,12H,5,10-11H2,1-2H3;1H
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Chemical Name |
3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride
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Synonyms |
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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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.04 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 25.0 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 (5.85 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 (5.85 mM) (saturation unknown) in 10% DMSO + 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 | 2.8143 mL | 14.0714 mL | 28.1429 mL | |
5 mM | 0.5629 mL | 2.8143 mL | 5.6286 mL | |
10 mM | 0.2814 mL | 1.4071 mL | 2.8143 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 |
NCT05190315 | Active Recruiting |
Radiation: Radiation Therapy Drug: Chlorpromazine Drug: Temozolomide |
Glioblastoma Multiforme | Mohammed Milhem | January 28, 2022 | Phase 1 |
NCT03021486 | Active Recruiting |
Drug: Chlorpromazine Drug: Haloperidol |
Delirium Advanced Malignant Neoplasm |
M.D. Anderson Cancer Center | June 5, 2017 | Phase 2 Phase 3 |
NCT01404364 | Completed | Drug: Triamcinolone Drug: Chlorpromazine |
Blind Painful Eye Refractory Glaucoma |
Hospital Governador Celso Ramos | January 2010 | Not Applicable |
NCT00202293 | Completed | Drug: Olanzapine Drug: Lithium Drug: Chlorpromazine |
Bipolar Disorder Schizoaffective Disorder |
Melbourne Health | October 1, 2001 | Phase 4 |
NCT03639558 | Completed | Drug: Haloperidol + Promethazine | Aggression Agitation |
Joseph Dib | August 28, 2018 | Phase 4 |