Pimozide-d4-1
Based on 1 Customer Validation
Pimozide-d4-1 is the deuterium labeled Pimozide. 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H25D4F2N3O
- Molecular Weight:465.57
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 2062-78-4
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Appearance Solid
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Molecular Weight 465.57
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Formel C28H25D4F2N3O
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Color White to off-white
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SMILES
O=C1NC2=C([2H])C([2H])=C([2H])C([2H])=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
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Synonyms
R6238-d4-1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : ≥ 30 mg/mL (64.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : ≥ 30 mg/mL (64.44 mM)
Ethanol : ≥ 3 mg/mL (6.44 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO / DMF | 1 mM | 2.1479 mL | 10.7395 mL | 21.4790 mL | 53.6976 mL |
| 5 mM | 0.4296 mL | 2.1479 mL | 4.2958 mL | 10.7395 mL | |
| DMSO / DMF | 10 mM | 0.2148 mL | 1.0740 mL | 2.1479 mL | 5.3698 mL |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4319 mL | 3.5798 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6849 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8592 mL | 2.1479 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7899 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3424 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0740 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL |