bexarotene

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和25 nM。它是一种类视黄醇类似物，用于治疗皮肤 T 细胞淋巴瘤的皮肤表现。

Bexarotene D4 is a deuterium-labeled Bexarotene (LGD1069). Bexarotene is a selective RXR agonist used in the treatment of cutaneous T-cell lymphoma.

6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.

Fluorobexarotene 是一种有效的 类视黄醇 X 受体 (RXR) 激动剂。Fluorobexarotene 对 RXRα 受体的 Ki 值为 12 nM，EC50 值为 43 nM。Fluorobexarotene 具有明显的 RXR 结合亲和力，比 Bexarotene 高75%。

OAB-14 是一种 Bexarotene 衍生物，通过清除 APP PS1 转基因小鼠的 β-淀粉样蛋白，改善其阿尔茨海默病相关的病理学和认知障碍。OAB-14 可有效改善 APP PS1 转基因小鼠内体自噬溶酶体（EAL）途径的功能障碍。