2806031-94-5
中文名稱
化合物 NIC-0102
英文名稱
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
2806031-94-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 NIC-0102 英文別名
Boronic acid, B-[(1R)-1-[[(2S)-2-[(2,6-difluorobenzoyl)amino]-1-oxo-3-phenylpropyl]amino]-3-methylbutyl]-物理化學(xué)性質(zhì)
密度1.235±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)9.67±0.43(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)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.