cyp11b1

BI 689648 is a highly selective inhibitor of aldosterone synthase(CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively).

Osilodrostat (LCI699) 是一种有效的人11β-羟化酶（CYP11B1）和醛固酮合成酶（CYP11B2）抑制剂，IC50分别值为2.5 和0.7nM，已获得 FDA 批准用于治疗库欣病。

CYP11B1-IN-2 (compound 7aa) 是一种选择性的、口服具有活力的 CYP11B1 抑制剂，能够作用于 human CYP11B1 (IC50: 9 nM) 和 rat CYP11B1 (IC50: 25 nM)。CYP11B1-IN-2 能够用于研究皮质醇过量所致疾病。

CYP11B2-IN-1 是一种有效的选择性 CYP11B2 抑制剂，对 CYP11B2 和 CYP11B1 的 IC50 分别为 2.3 nM 和 142 nM。

Tetrahydro-11-deoxy cortisol (THS) is the primary urinary metabolite of 11-deoxycortisol. Urinary excretion of THS is elevated in patients with 11β-hydroxylase deficiency, a condition resulting from mutations in the cytochrome P450 (CYP) isoform CYP11B1. Urinary levels of THS are also elevated in patients with adrenocortical carcinoma (ACC) and adrenocortical adenoma (ACA) but are higher in patients with ACC compared to ACA.

CYP11B2-IN-2 (Compound 10k) 作为醛固酮合酶CYP11B2的有效抑制剂，其IC50值仅为 0.3 nM。此外，CYP11B2-IN-2 还可开发成18F 标记的正电子发射断层扫描 (PET) 示踪剂，用于检测和诊断原发性醛固酮症。