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Chlorpromazine HCl Dopamine Receptor inhibitor

Cat.No.S2456

Chlorpromazine HCl is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.
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Quality Control

Batch: Purity: 99.96%
99.96

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells Function assay Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in cloned CHO cells, Ki=0.673 μM
CHO cells Function assay Compound was evaluated for the binding affinity against [3H]U-86,170-labeled D2 sites in cloned CHO cells, Ki=0.003 μM
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Solubility

In vitro
Batch:

DMSO : 71 mg/mL (199.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 71 mg/mL

Ethanol : 71 mg/mL

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 355.33 Formula

C17H19ClN2S.HCl

Storage (From the date of receipt)
CAS No. 69-09-0 Download SDF Storage of Stock Solutions

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Dopamine receptor
Potassium channel
In vitro
Chlorpromazine affects miniature IPSCs (mIPSCs) by decreasing the binding (kon) and by increasing the unbinding (koff) rates of GABAARs. Chlorpromazine modulates activated TRPA1 currents in a voltage-dependent way, leading to a block at positive potentials and an increased open probability at negative potentials.
In vivo
Chlorpromazine independently down-regulates the production of various T cell-derived lymphokines (IL-2, IFN-gamma, IL-4, TNF, and GM-CSF) and up-regulates the secretion of IL-10 in an in vivo model of acute superantigen-driven immune activation. Chlorpromazine -mediated amplification of the SEB-driven Chlorpromazine secretion is accompanied by an enhanced IL-10 mRNA accumulation. Chlorpromazine protects mice, normal or adrenalectomized, and guinea pigs against lethality of LPS, and inhibits TNF serum levels. Chlorpromazine protects against LPS lethality when administered 30 minutes (min) before, simultaneously, or up to 10 min after LPS and is ineffective when given 30 min after LPS, paralleling the inhibitory effect on TNF production. Chlorpromazine significantly inhibits LPS lethality and hepatotoxicity in mice sensitized to LPS toxicity by actinomycin D, whereas under these conditions DEX is inactive. Chlorpromazine protects brain tissue from hypoxia-induced irreversible loss of synaptic transmission in rats. Chlorpromazine also significantly delays the occurrence of the hypoxia-induced spreading depression (SD) in rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/2033366/
  • [5] https://pubmed.ncbi.nlm.nih.gov/3022872/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-11-18)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05431595 RECRUITING
Delirium; Epileptics; Neuroleptics
M.D. Anderson Cancer Center
2022-07-19 PHASE2; PHASE3
NCT07364344 NOT_YET_RECRUITING
Acute Ischemic Stroke
Ji Xunming,MD,PhD
2026-01
NCT06663631 RECRUITING
Acute Ischemic Stroke
Capital Medical University
2024-11-09 PHASE1
NCT06238089 Recruiting
Intellectual Disability
University of Plymouth|Peninsula Clinical Trials Unit
2023-12-19 --
NCT05190315 COMPLETED
Glioblastoma Multiforme
Mohammed Milhem
2022-01-28 PHASE1
NCT05433402 WITHDRAWN
Colon Cancer Stage III
Sadat City University
2022-07-20 PHASE1; PHASE2

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