CAS Number2062-78-4
Synonymspimozida; 1-[4,4-Di-(4-fluorophenyl)butyl]-4-(2-oxo-1-benzimidazolinyl)piperidine; Neoperidole; Pimozidum; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidinyl}-1,3-dihydro-2H-benzimidazol-2-one; pimozide; 1-[1-[4,4-bis(4-Fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one; EINECS 218-171-7; 3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one; 1-[1-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-2-benzimidazolinone; Orap; McN-JR-6238; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidinyl}-1H-benzimidazol-2-ol; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one; Opiran; MFCD00055081
Molecular FormulaC28H29F2N3O
Molecular Weight461.55
Purity98.00%
Density1.2±0.1 g/cm3
Boiling Point649.0±65.0 °C at 760 mmHg
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 2062-78-4 |
| Catalog No. | 2A-9027930 |
| Chinese Name | 匹莫齐特 |
| Synonyms | pimozida; 1-[4,4-Di-(4-fluorophenyl)butyl]-4-(2-oxo-1-benzimidazolinyl)piperidine; Neoperidole; Pimozidum; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidinyl}-1,3-dihydro-2H-benzimidazol-2-one; pimozide; 1-[1-[4,4-bis(4-Fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one; EINECS 218-171-7; 3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one; 1-[1-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-2-benzimidazolinone; Orap; McN-JR-6238; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]-4-piperidinyl}-1H-benzimidazol-2-ol; 1-{1-[4,4-Bis(4-fluorophenyl)butyl]piperidin-4-yl}-1,3-dihydro-2H-benzimidazol-2-one; Opiran; MFCD00055081 |
| Molecular Formula | C28H29F2N3O |
| Molecular Weight | 461.55 |
| Purity | 98.00 |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 649.0±65.0 °C at 760 mmHg |
| Water Solubility | DMSO: 18 mg/mL |
| Storage Condition | Sealed, store at 2 ºC -8 ºC |
| Packaging | III |
| Application | Pimozide is an antagonist of dopamine receptors, with Ki values of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors respectively. It also has high affinity for α1-adrenoceptor with a K |
| HTC | 2933990090 |
| PubChem ID | 9769 |
| SMILES | O=c1[nH]c2ccccc2n1C1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 |
| InChI | InChI=1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34) |
| InChI Key | YVUQSNJEYSNKRX-UHFFFAOYSA-N |
| Hazard Symbols | 6.1(b) |
| Bioactivity | 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. Related Catalog Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Signaling Pathways >> JAK/STAT Signaling >> STAT Signaling Pathways >> Stem Cell/Wnt >> STAT Research Areas >> Cancer Research Areas >> Neurological Disease Target Dopamine D2 receptor:1.4 nM (Ki) Dopamine D3 receptor:2.5 nM (Ki) Dopamine D1 receptor:588 nM (Ki) α1-adrenoceptor:39 nM (Ki) STAT3 STAT5 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]. 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]. References [1]. Ybema CE, et al. Adrenoceptors and dopamine receptors are not involved in the discriminative stimulus effect of the 5-HT1A receptor agonist flesinoxan. Eur J Pharmacol. 1994 Apr 21;256(2):141-7. [2]. Cai N, et al. The STAT3 inhibitor pimozide impedes cell proliferation and induces ROS generation in human osteosarcoma by suppressing catalase expression. Am J Transl Res. 2017 Aug 15;9(8):3853-3866. eCollection 2017. [3]. Erik A. Nelson, et al. The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors. Blood. 2011 Mar 24; 117(12): 3421-3429. Chemical & Physical Properties Density 1.2±0.1 g/cm3 Boiling Point 649.0±65.0 °C at 760 mmHg Molecular Formula C28H29F2N3O Molecular Weight 461.546 Flash Point 346.3±34.3 °C Exact Mass 461.227875 PSA 41.03000 LogP 6.06 Vapour Pressure 0.0±2.0 mmHg at 25°C Index of Refraction 1.623 InChIKey YVUQSNJEYSNKRX-UHFFFAOYSA-N SMILES O=c1[nH]c2ccccc2n1C1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 Storage condition 2-8°C Water Solubility DMSO: 18 mg/mL |
| Use of | 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. Properties Articles57 Name pimozide Synonym More Synonyms pimozide Biological Activity 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; Pimozide also inhibits STAT3 and STAT5. Related Catalog Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Signaling Pathways >> JAK/STAT Signaling >> STAT Signaling Pathways >> Stem Cell/Wnt >> STAT Research Areas >> Cancer Research Areas >> Neurological Disease Dopamine D2 receptor:1.4 nM (Ki) Dopamine D3 receptor:2.5 nM (Ki) Dopamine D1 receptor:588 nM (Ki) α1-adrenoceptor:39 nM (Ki) References [1]. Ybema CE, et al. Adrenoceptors and dopamine receptors are not involved in the discriminative stimulus effect of the 5-HT1A receptor agonist flesinoxan. Eur J Pharmacol. 1994 Apr 21;256(2):141-7. [2]. Cai N, et al. The STAT3 inhibitor pimozide impedes cell proliferation and induces ROS generation in human osteosarcoma by suppressing catalase expression. Am J Transl Res. 2017 Aug 15;9(8):3853-3866. eCollection 2017. [3]. Erik A. Nelson, et al. The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors. Blood. 2011 Mar 24; 117(12): 3421-3429. Chemical & Physical Properties Molecular Formula C28H29F2N3O Exact Mass 461.227875 PSA 41.03000 Index of Refraction 1.623 InChIKey YVUQSNJEYSNKRX-UHFFFAOYSA-N |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Purity: 98.0% |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: Non-dangerous goods IMDG Code: Non-dangerous goods International air transport dangerous goods regulations: non-dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special reminder to users No data available |
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