5-[4-フェニル-5-(トリフルオロメチル)-2-チエニル]-3-[3-(トリフルオロメチル)フェニル]-1,2,4-オキサジアゾール 化学特性,用途語,生産方法
説明
Sphingosine-
1-
phosphate receptor 1 (S1P
1) is one of five high affinity G protein-
coupled S1P receptors which mediate a variety of effects including lymphocyte recirculation in the blood. Non-
selective S1P receptor agonists, such as FTY720, produce clinical immunosuppression useful for preventing transplant rejection and treating autoimmune diseases. However, they also cause bradycardia by activating S1P
3, the receptor responsible for regulation of heart rate. SEW2871 is a selective S1P
1 receptor agonist in both human and mouse that is not active at the S1P
2-5 receptors. SEW2871, therefore, suppresses the immune response by decreasing the number of lymphocytes circulating in blood without causing bradycardia.
使用
5-[4-PHENYL-5-(TRIFLUOROMETHYL)-2-THIENYL]-3-[3-(TRIFLUOROMETHYL)PHENYL]-1,2,4-OXADIAZOLE is used as medicament for treating and/or preventing cardiovascular conditions in patients with Fabry disease.
生物活性
Novel, potent and selective sphingosine-1-phosphate 1 (S1P 1 ) receptor agonist. Activates S1P 1 receptor with an EC 50 of 13 nM, but does not activate S1P 2 , S1P 3 , S1P 4 or S1P 5 receptors at concentrations up to 10 μ M. Cell-permeable and active in vivo .
5-[4-フェニル-5-(トリフルオロメチル)-2-チエニル]-3-[3-(トリフルオロメチル)フェニル]-1,2,4-オキサジアゾール 上流と下流の製品情報
原材料
準備製品