147776-06-5
中文名稱
L-161,982
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T15681化合物L-161982
英文別名
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-
物理化學性質(zhì)
密度1.37±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO：可溶15mg/mL，澄清
酸度系數(shù)(pKa)4.57±0.10(Predicted)
形態(tài)粉末
顏色白色至米色
InChIKeyMMDNKTXNUZFVKD-UHFFFAOYSA-N
SMILESFC(F)(F)c1c(cccc1)[n]2nc([n]([c]2=O)Cc3ccc(cc3)c4c(cccc4)[S](=O)(=O)NC(=O)c5[s]ccc5C)CCCC
常見問題列表
生物活性
L-161982 是一種選擇性的 EP4 受體拮抗劑。L-161982 完全阻斷 PGE2 誘導的 HCA-7 細胞 ERK 磷酸化和細胞增殖。L-161982 減輕膠原誘導的小鼠關(guān)節(jié)炎。靶點
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EP4
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體外研究
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. |
體內(nèi)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. |