1. GPCR/G Protein
    Neuronal Signaling
    JAK/STAT Signaling
    Stem Cell/Wnt
  2. Dopamine Receptor
    Adrenergic Receptor

Pimozide (Synonyms: R6238)

目录号: HY-12987 纯度: 99.88%

Pimozide 是 dopamine receptor 的拮抗剂,对 dopamine D2,D3 和 D1 受体的 Ki 值分别为 1.4 nM,2.5 nM 和 588 nM,同时对 α1-adrenoceptor 也有较高亲和性,Ki 值为 39 nM;Pimozide 也是 STAT3STAT5 的抑制剂。

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Pimozide Chemical Structure

Pimozide Chemical Structure

CAS No. : 2062-78-4

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥550 In-stock
50 mg ¥500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.

IC50 & Target[1][2][3]

Dopamine D2 receptor

1.4 nM (Ki)

Dopamine D3 receptor

2.5 nM (Ki)

Dopamine D1 receptor

588 nM (Ki)


39 nM (Ki)





In Vitro

Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively; also has affinity at α1-adrenoceptor and 5-HT1A, with Kis of 39 nM and 310 nM, respectively[1]. Pimozide acts as an inhibitor of STAT3. Pimozide (0-15 μM) shows inhibitory of the proliferation of U2OS cells, with IC50 value at 24, 48, and 72 h of 22.16 ± 2.54, 17.49 ± 1.14 and 13.78 ± 0.34 μM, respectively. Pimozide (10 μM) inhibits the colony- and sphere-forming abilities of osteosarcoma cells. Pimozide (15 μM) induces G0/G1 phase cell cycle arrest, suppresses the extracellular signal-regulated kinase (Erk) signaling to inhibit cell viability, and produces ROS generation through inhibiting antioxidant enzyme gene catalase expression in osteosarcoma cells[2]. Pimozide acts as an inhibitor of STAT5. Pimozide reduces the expression of endogenous STAT5 target genes, and decreases STAT5 tyrosine phosphorylation[3].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (72.21 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1666 mL 10.8331 mL 21.6661 mL
5 mM 0.4333 mL 2.1666 mL 4.3332 mL
10 mM 0.2167 mL 1.0833 mL 2.1666 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

Cell Assay

Cell proliferation is assessed by WST-8 colorimetric assay. Human osteosarcoma cells are plated in 96-well plates with 2,500 cells per well and exposed to the treatment of different concentrations of pimozide for various time intervals (24 h, 48 h, and 72 h). The WST-8 solution is added to each well after indicated time. After incubated at 37°C for another 4 hours, the absorbance ismeasured at 450 nm using a multi-well plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Purity: 99.88%

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Cat. No.: HY-12987