N-[[4′-[[3-ブチル-1,5-ジヒドロ-5-オキソ-1-[2-(トリフルオロメチル)フェニル]-4H-1,2,4-トリアゾール-4-イル]メチル]-2-ビフェニリル]スルホニル]-5-メチル-2-チオフェンカルボアミド 化學(xué)特性,用途語,生産方法
説明
Prostaglandin E
2 (PGE
2) exerts its effects through four separate G coupled-
protein receptors (EP
1-4). L-
161,982 is a potent and selective EP
4 receptor antagonist. It demonstrates selective binding to human EP
4 receptors with a K
i value of 0.024 μM compared to other receptors of the prostanoid family, EP
1, EP
2, EP
3, DP, FP, and IP, with K
i values of 17, 23, 1.9, 5.1, 5.6, and 6.7 μM, respectively. L-
161,982 at 10 mg/kg/day suppresses PGE
2-
stimulated bone formation in young rats and at 100 nM reverses the anti-
inflammatory action of PGE
2 in LPS-
activated human macrophages. At 10 μM L-
161982 blocks PGE
2-
induced cell proliferation in HCA-
7 colon cancer cells.
使用
L-161,982 is an EP4 receptor antagonist, which blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells.
生物活性
EP 4 receptor antagonist that is selective over all other members of the prostanoid receptor family (K i values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μ M for human EP 4 , TP, EP 3 , DP, FP, IP, EP 1 and EP 2 receptors respectively). Suppresses PGE 2 -induced bone formation in rats and prevents the nociceptive response induced by misoprostol in formalin-injected mice.
N-[[4′-[[3-ブチル-1,5-ジヒドロ-5-オキソ-1-[2-(トリフルオロメチル)フェニル]-4H-1,2,4-トリアゾール-4-イル]メチル]-2-ビフェニリル]スルホニル]-5-メチル-2-チオフェンカルボアミド 上流と下流の製品情報
原材料
準備製品