| Bioactivity | CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 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]. |
| Invitro | 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 IC50 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]. |
| In Vivo | 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: |
| Name | CYP11B1-IN-2 |
| Formula | C21H19N5O2 |
| Molar Mass | 373.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yin L, et al. Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[d]isoxazoles as Potent and Selective Inhibitors of 11β-Hydroxylase. J Med Chem. 2022 Aug 17. |