Product Description: 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[1][2][3][4].
Applications: Metabolism-protein/nucleotide metabolism
Formula: C28H25D4F2N3O
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. /[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.
Molecular Weight: 465.57
Compound Purity: 99.68
Research Area: Cancer; Endocrinology; Neurological Disease
Solubility: 10 mM in DMSO/DMF : ≥ 30mg/mL/DMSO : ≥ 30mg/mL/Ethanol : ≥ 3mg/mL
Target: Adrenergic Receptor;Dopamine Receptor;Parasite;STAT
English
Deutsch
