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

Pimozide (Synonyms: R6238)

目录号: HY-12987 纯度: 98.01%
产品使用指南

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;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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Description

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; also inhibits STAT3 and STAT5.

IC50 & Target

Ki: 1.4 nM (Dopamine D2 receptor), 2.5 nM (Dopamine D3 receptor), 588 nM (Dopamine D1 receptor), 39 nM (α1-adrenoceptor), 310 nM (5-HT1A)[1]
STAT3[2], STAT5[3]

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].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[2]

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.

References
Molecular Weight

461.55

Formula

C₂₈H₂₉F₂N₃O

CAS No.

2062-78-4

SMILES

O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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