ar-7

AR7 是一种非典型的 RARA RARα(视黄酸受体 α) 拮抗剂，能够特异性激活伴侣介导的自噬活性，对自噬无影响。

SAR-7226 Hydrate, a SGLT1 2 inhibitor, is used potentially for the treatment of type 2 diabetes.

SAR7334 hydrochloride, a potent and specific inhibitor of TRPC6 (IC50 of 7.9 nM), effectively targets and inhibits the TRPC6 channel.

SAR7334 (TRCP6-IN-1) 是 TRPC6特异性抑制剂，抑制 TRPC6 电流的 IC50为 7.9 nM。

Dodecapeptide AR71 作为黑色素瘤抑制活性 (MIA) 的有效抑制剂，具有降低细胞迁移、减少转移形成和增强免疫反应的功能。该化合物主要被用于恶性黑色素瘤治疗的研究中。

E3ligaseLigand 44 是一种用于合成 PROTAC AR Degrader-7 的 E3 连接酶配体。

AR ligand-32是一种靶蛋白配体，专用于合成PROTAC AR Degrader-7。

XYD049 (compound 7d) 是一种CRBN型分子胶，专门靶向GSPT1，具有DC50为19 nM的效能，用于研究由MYC驱动的去势抵抗性前列腺癌（CRPC）。XYD049 有效抑制22Rv1细胞的生长，IC50为7 nM，并在体内表现出抗肿瘤活性。通过下调22Rv1细胞中的CRPC相关癌基因，包括AR、AR-v7、PSA和c-Myc，XYD049 展现其作用机制。此化合物由分子胶的linker (black part) NH2-C5-NH-Boc、CRBN型E3连接酶配体 (blue part) Thalidomide 4-fluoride，以及靶蛋白配体 (red part) GSPT1 ligand-1 组成，其中E3连接酶配体与linker 形成偶联物E3 Ligase Ligand-linker Conjugate 158。

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

LL-K9-3是一种基于选择性疏水标记技术（HyT）的CDK9-cyclin T1复合物降解剂（DC50值分别为cyclin T1的589 nM和CDK9的662 nM）。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs（CDK1、2、4、5、6和7）。在22RV1细胞中，LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解，降低雄激素受体（AR）和cMyc的表达。

AR antagonist 7 (86) 是一种雄激素受体 (AR) 拮抗剂，可用于脱发研究。

3,4-Dihydro-6,7-isoquinolinediol (compound 7) 作为β2-AR的激动剂，在 CH-K1 GA1S 细胞中显示出 EC50 值为 106.9 μM。此外，该化合物还能抑制 LPS 诱导的小鼠巨噬细胞 RAW 264.7 中 NO 的产生，表现出抗炎活性。