147776-06-5
中文名称
L-161,982
英文名称
L-161,982
CAS
147776-06-5
分子式
C32H29F3N4O4S2
分子量
654.72
MOL 文件
147776-06-5.mol
更新日期
2023/03/17 20:03:07
147776-06-5 结构式
基本信息
中文别名
化合物 T15681化合物L-161982
英文别名
L-161,982L-161,982 >=98% (HPLC)
N-[2-[4-[[3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonyl-3-methylthiophene-2-carboxamide
N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]- 2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
2-Thiophenecarboxamide, N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-
常见问题列表
生物活性
L-161982 是一种选择性的 EP4 受体拮抗剂。L-161982 完全阻断 PGE2 诱导的 HCA-7 细胞 ERK 磷酸化和细胞增殖。L-161982 减轻胶原诱导的小鼠关节炎。靶点
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EP4
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体外研究
L-161982 (10 μM; 2 hours) blocks PGE2-stimulated cell proliferation of HCA-7 cells.
L-161982 (10 μM; 1 hour) blocks PGE2-stimulated ERK phosphorylation in HCA-7 cells.
L-161982 induces apoptosis, cell cycle arrest, and inhibits prostaglandin E2-induced proliferation in oral squamous carcinoma Tca8113 cells.
Cell Proliferation Assay
| Cell Line: | HCA-7 cells |
| Concentration: | 10 μM |
| Incubation Time: | 2 hours |
| Result: | Blocked PGE2-induced cell proliferation. |
体内研究
L-161982 (5 mg/kg; i.p.; once per day for 2 weeks) reduces arthritis lesions and lesion progression in CIA mice.
| Animal Model: | Female DBA/1 mice of 6 to 8 weeks old (collagen-induced arthritis (CIA) mice model) |
| Dosage: | 5 mg/kg |
| Administration: | i.p.; once per day for 2 weeks |
| Result: | Showed less joint swelling and lower arthritis score after 35 days post immunization. |