| Bioactivity | hCES2A-IN-1 (compound 20w) is a potent hCES2A inhibitor, with an IC50 value of 1.6 nM. hCES2A-IN-1, a bysspectin A derivative, shows an approximately 1000-fold improvement over the lead compound bysspectin A[1]. |
| Target | hCES2A (0.0016 ± 0.00034 μM), hCES1A (7.26 ± 0.94 μM) |
| Invitro | hCES2A-IN-1 (compound 20w) 在浓度低于 10 μM 时对 HepG2 细胞表现出非常弱的细胞毒性[1]。hCES2A-IN-1 能够以剂量依赖性方式抑制活细胞中 hCES2A 介导的 NCEN 水解，IC50 值为 0.052 μM，其抑制活性显着高于 Loperamide，IC50 值为 1.44 μM[1]。hCES2A-IN-1 表现出良好的代谢稳定性，在人肝微粒体I相或II相代谢系统中的半衰期分别为125.96分钟和97.38分钟[1]。 0 --> hCES2A-IN-1 相关抗体: |
| Name | hCES2A-IN-1 |
| Formula | C23H26O4 |
| Molar Mass | 366.45 |
| 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]. Li W, et al. New bysspectin A derivatives as potent inhibitors of human carboxylesterase 2A. Eur J Med Chem. 2023 Nov 5;259:115708. |