Pimozide

Synonyms: Orap, R6238

Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.

Pimozide Chemical Structure

Pimozide Chemical Structure

CAS: 2062-78-4

Selleck's Pimozide has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Pimozide Related Products

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Biological Activity

Description Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Targets
STAT3 [1] STAT5 [2] Dopamine D3 receptor [3]
(Cell-free assay)
Dopamine D2 receptor [3]
(Cell-free assay)
α1-adrenoceptor [3]
(Cell-free assay)
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0.83 nM(Ki) 3.0 nM(Ki) 39 nM(Ki)
In vitro
In vitro

Pimozide, a STAT5 inhibitor, has no effect on prolactin-induced ERα phosphorylation.[4]

Cell Research Cell lines MMQ rat prolactinoma cell line
Concentrations 5 µM
Incubation Time --
Method

MMQ cells were treated with PRL (20 ng/ml) in the absence and presence of the JAK2 inhibitor AG-490 (50 μM), the PI3K inhibitor wortmannin (0.5 µM), the MEK inhibitor U0126 (10 µM) or the STAT5 inhibitor pimozide (5 µM).

(Data sourced from selleck products)

Chemical Information & Solubility

Molecular Weight 461.55 Formula

C28H29F2N3O

CAS No. 2062-78-4 SDF Download Pimozide SDF
Smiles FC1=CC=C(C=C1)C(CCCN2CCC(CC2)N3C(=O)NC4=CC=CC=C34)C5=CC=C(F)C=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (194.99 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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