CYP11B1-IN-2 (compound 7aa) 是一种口服有效且选择性的CYP11B1抑制剂，其对 human CYP11B1 和 rat CYP11B1 的IC50值分别为 9 nM 和 25 nM。CYP11B1-IN-2 可用于皮质醇过量所致疾病的研究。

CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC 50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol [1].

CYP11B1-IN-2 (compound 7aa) exhibits good selectivity over a panel of hepatic CYP enzymes, such as CYP1A2, CYP2C9, CYP2C19, CYP3A4, CYP2D6, and CYP2E1 with IC 50 values greater than 10 μM [1]. CYP11B1-IN-2 presents a cLog P of 3.12, indicating a good balance between lipophilicity and hydrophilicity, which was further manifested by an aqueous solubility of 196 μM [1].

CYP11B1-IN-2 (compound 7aa) (25 mg/kg, Orally, once) reduces plasma cortisol concentrations in rats [1]. CYP11B1-IN-2 (5 mg/kg (IV) or 25 mg/kg (Orally); once) has a maximum plasma concentration of 12 686 μg/L, with similar terminal half-lives of around 4.5 h [1]. Animal Model: Adult Sprague-Dawley rats (male, 250-300 g) [1] Dosage: 25 mg/kg Administration: Orally, once Result: Strongly reduced the plasma concentrations of cortisol from 376 ± 22 to 28 ± 5 ng/L after a dose of 25 mg/kg body weight per oral in rats. Animal Model: Adult Sprague-Dawley rats (male, 250-300 g) [1] Dosage: 5 mg/kg (IV) or 25 mg/kg (Orally) Administration: IV or Orally, once Result: Pharmacokinetic Parameters of CYP11B1-IN-2 in male Sprague-Dawley rats [1]. IV (5 mg/kg) PO (25 mg/kg) T max (h) 0 4.2 ± 0.2 C max (μg/L) 12 685.7 ± 421.3 7993.3 ± 478.7 AUC 0-∞ (μg/L·h) 50 928.7 ± 982.6 54 539.2 ± 1633.9 T 1/2 (h) 4.5 ± 0.4 4.6 ± 0.2 CL (mL/h/kg) 17.2 ± 1.2 F (%) 21.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years