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Pimozide-d5 N-Oxide

CAT: 0804-HY-12987S1-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12987S1-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Pimozide-d5 N-Oxide 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].
CAS Number
1794795-40-6
UNSPSC
12352005
Target
Adrenergic Receptor; Dopamine Receptor; Isotope-Labeled Compounds; STAT
Type
Isotope-Labeled Compounds
Related Pathways
GPCR/G Protein; JAK/STAT Signaling; Neuronal Signaling; Others; Stem Cell/Wnt
Field of Research
Cancer; Neurological Disease; Endocrinology
Solubility
10 mM in DMSO
Smiles
O=C1N(C=2C(N1)=CC=CC2)C3(C(CN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)(=O)CC3([2H])[2H])([2H])[2H])[2H]
Molecular Formula
C28H24D5F2N3O2
Molecular Weight
482.58
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Isoform
D1 Receptor; D3 Receptor