1003019-41-7
中文名稱
GNF362
英文名稱
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 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)623.9±55.0 °C(Predicted)
密度1.38±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 125 mg/mL (293.12 mM)
酸度系數(shù)(pKa)13.04±0.50(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
GNF362 是肌醇三磷酸3'激酶 B (Itpkb) 的選擇性，有效且可口服生物利用的抑制劑，IC50為 9 nM。 GNF362 還抑制 Itpka 和 Itpkc，IC50 值分別為 20 nM 和 19 nM。 肌醇三磷酸3'激酶 B (Itpkb) 是一種 Ca2+ 依賴性激酶，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]。體外研究
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.
體內(nèi)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. |