Pimozide-d4(Synonyms: R6238-d4)

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Pimozide-d4 (Synonyms: R6238-d4)

Pimozide D4 (SKI-606 D8) 是 Pimozide 的氘代物。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；Pimozide 也是 STAT3 和 STAT5 的抑制剂。

Pimozide-d4(Synonyms: R6238-d4)

Pimozide-d4 Chemical Structure

CAS No. : 1803193-57-8

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生物活性

Pimozide D4 (R6238 D4) is a 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].

IC50 & Target

STAT3

 

STAT5

 

Dopamine D2 receptor

1.4 nM (Ki)

opamine D3 receptor

2.5 nM (Ki)

opamine D1 receptor

588 nM (Ki)

α1-adrenoceptor

39 nM (Ki)

Clinical Trial

分子量

465.57

Formula

C28H25D4F2N3O
CAS 号

1803193-57-8
中文名称

匹莫齐特 d4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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