L-161,982
| 中文名称 | L-161,982 |
|---|---|
| 中文同义词 | 化合物 T15681;化合物L-161982 |
| 英文名称 | L-161,982 |
| 英文同义词 | L-161,982;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;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;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-;L-161,982 >=98% (HPLC);colon,cancer,phosphorylation,prostaglandin,Prostaglandin Receptor,L161982,arthritis,inhibit,proliferation,L 161982,L-161982,Inhibitor |
| CAS号 | 147776-06-5 |
| 分子式 | C32H29F3N4O4S2 |
| 分子量 | 654.72 |
| EINECS号 | |
| 相关类别 | Prostanoid receptor and related |
| Mol文件 | 147776-06-5.mol |
| 结构式 |  |
L-161,982 性质
| 密度 | 1.37±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 酸度系数(pKa) | 4.57±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
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。
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EP4
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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. |
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. |
安全信息
| WGK Germany | 3 |
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