1003019-41-7
中文名称
GNF362
英文名称
GNF362
CAS
1003019-41-7
分子式
C22H21F3N6
分子量
426.44
MOL 文件
1003019-41-7.mol
更新日期
2023/03/20 15:41:27
1003019-41-7 结构式
常见问题列表
生物活性
GNF362 是肌醇三磷酸3'激酶 B (Itpkb) 的选择性，有效且可口服生物利用的抑制剂，IC50为 9 nM。 GNF362 还抑制 Itpka 和 Itpkc，IC50 值分别为 20 nM 和 19 nM。 肌醇三磷酸3'激酶 B (Itpkb) 是一种 Ca2+ 依赖性激酶，其磷酸化 Ins (1,4,5) P3 的 3' 位置，生成肌醇 1,3,4,5-四磷酸 [Ins (1,3,4,5) P4]。体外研究
GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca 2+ responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes. GNF362 augments SOC responses following antigen receptor cross-linking, with an EC 50 of 12 nM in primary B or T lymphocytes.
体内研究
GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg.
| Animal Model: | A Lewis rat antigen-induced arthritis (rAIA) model |
| Dosage: | 6 or 20 mg/kg |
| Administration: | Orally administration; 6 or 20 mg/kg; twice daily; 21 days |
| Result: | Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively. |