Bexarotene-d3(Synonyms: 贝沙罗汀 d3)

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Bexarotene-d3 (Synonyms: 贝沙罗汀 d3)

Bexarotene-d3 (LGD1069-d3) 是 Bexarotene 的氘代物。Bexarotene (LGD1069) 是一种高亲和力的选择性类视黄醇 X 受体 (RXR) 激动剂，对 RXRα、RXRβ 和 RXRγ 的 EC50 分别为 33、24、25 nM。Bexarotene 对 RAR 受体的亲和力有限 (EC50 >10000 nM)。Bexarotene 可用于皮肤 T 细胞淋巴瘤的研究。

Bexarotene-d3(Synonyms: 贝沙罗汀 d3)

Bexarotene-d3 Chemical Structure

CAS No. : 166175-35-5

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生物活性

Bexarotene-d3 (LGD1069-d3) is the deuterium labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma[1][2][3][4].

体外研究
(In Vitro)

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

351.50

Formula

C24H25D3O2
CAS 号

166175-35-5
中文名称

贝沙罗汀 d3
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nathalia Rodrigues de Almeida, et al.  A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.

    [3]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886.

    [4]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9.

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