2806031-94-5
中文名称
化合物 NIC-0102
英文名称
Boronic acid, B-[(1R)-1-[[(2S)-2-[(2,6-difluorobenzoyl)amino]-1-oxo-3-phenylpropyl]amino]-3-methylbutyl]-
CAS
2806031-94-5
分子式
C21H25BF2N2O4
分子量
418.24
MOL 文件
2806031-94-5.mol
结构式
基本信息
中文别名
化合物 NIC-0102
英文别名
Boronic acid, B-[(1R)-1-[[(2S)-2-[(2,6-difluorobenzoyl)amino]-1-oxo-3-phenylpropyl]amino]-3-methylbutyl]-
物理化学性质
| 密度 | 1.235±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 9.67±0.43(Predicted) |
| 形态 | Solid |
| 颜色 | White to off-white |
应用领域
用途一
NIC-0102 is an orally bioavailable proteasome inhibitor. NIC-0102 specifically prevents NLRP3 inflammasome activation but has no effect on NLRC4 or AIM2 inflammasomes. In vitro studies revealed that NIC-0102 induced the polyubiquitination of NLRP3, interfered with the NLRP3?ASC interaction, and blocked ASC oligomerization, thereby resulting in the inhibition of NLRP3 inflammasome activation. In addition, NIC-0102 also inhibited the production of pro-IL-1β. Importantly, NIC-0102 showed potent anti-inflammatory effects on DSS-induced ulcerative colitis model in vivo.