non-steroidal androgen receptor (AR) antagonist

Leelamine hydrochloride, a tricyclic diterpene extracted from pine tree bark, inhibits the transcriptional activity of the androgen receptor, known to regulate fatty acid synthesis [2,3]. This compound acts as a cannabinoid receptor type 1 (CB1) agonist and suppresses SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells, irrespective of androgen receptor status.

Enclomiphene ((E)-Clomiphene) hydrochloride 是一种口服具有活力的、有效的非甾体雌激素受体 (estrogen receptor) 拮抗剂，具有抗雌激素作用。Enclomiphene hydrochloride 能够用于研究卵巢功能障碍、睾酮缺乏、男性性腺功能减退症和 type 2 型糖尿病。

DK3 是雌激素相关受体 α(ERRα)的一种有效的选择性激动剂，ERRα是癌症和代谢性疾病的潜在药物靶点[1]。

Cholesterol-d4 是 Cholesterol 的氘代化合物。Cholesterol 的 CAS 号为 57-88-5。Cholesterol 是哺乳动物中的主要固醇，占质膜结构成分的 20-25％。Cholesterol 在确定膜的流动性和渗透性特征以及转运蛋白和信号蛋白的功能中起着重要作用。Cholesterol 还是内源性雌激素相关受体 α 激动剂。

OP-1074 is a pure antiestrogen and a selective degrader of ER, shows specific antiestrogenic activity for ERα and ERβ.

(1S,3R)-GNE-502 (compound 179) 是一种 Erα 的有效降解剂，能够在 MCF7 HCS 细胞中降解 ERα (EC50: 13 nM)。(1S,3R)-GNE-502 可以用于与雌激素受体相关癌症的研究。

GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.

DK1 是有效的雌激素相关受体调节剂。DK1 影响 ERRα 受体的活性，具有降低血糖的能力。DK1 显示出研究糖尿病的潜力。