General description
一种有效的免疫调节剂,能抑制IL-15刺激CD4 T细胞后的IL-17生成。
Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. IC50 value: 20-60 nM (IL-17 production) . Target: IL-17 Y-320 inhibited IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Oral administration of Y-320 (0.3 to 3 mg/kg) significantly inhibited the development and progression of arthritis and joint destruction with reduction of IL-17 mRNA expression in arthritic joints of type II collagen-induced arthritis (CIA) in DBA/1J mice. Y-320 in combination with anti-murine tumor necrosis factor-α monoclonal antibody showed a synergistic effect on mouse CIA. Moreover, therapeutic treatment with Y-320 (0.3 and 1 mg/kg orally) ameliorated CIA in cynomolgus monkeys .
Y-320是一种新型的苯基吡唑苯胺内酯免疫调节剂; 抑制由IL-15刺激的CD4 T细胞的IL-17产生,IC50值为20至60 nM。 IC50值:20-60 nM(IL-17生产)。 靶标:IL-17 Y-320抑制了用IL-15刺激的CD4 T细胞的IL-17产生,IC50值为20至60 nM。 口服Y-320(0.3至3 mg / kg)可显着抑制关节炎的发展和进展以及关节破坏,并降低DBA / 1J的II型胶原诱导的关节炎(CIA)关节炎关节中IL-17 mRNA的表达。 老鼠。 Y-320联合抗鼠肿瘤坏死因子-α单克隆抗体对小鼠CIA具有协同作用。 此外,用Y-320(0.3和1 mg / kg口服)进行的治疗改善了食蟹猴的CIA。
Properties
Iupac Name: | 1-(4-chlorophenyl)-N-(3-cyano-4-(4-morpholinopiperidin-1-yl)phenyl)-5-methyl-1H-pyrazole-4-carboxamide |
Inchi Code | 1S/C27H29ClN6O2/c1-19-25(18-30-34(19)24-5-2-21(28)3-6-24)27(35)31-22-4-7-26(20(16-22)17-29)33-10-8-23(9-11-33)32-12-14-36-15-13-32/h2-7,16,18,23H,8-15H2,1H3,(H,31,35) |
Inchi Key | BWZNJVZTAWBIFG-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport