Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.

  title={Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.},
  author={Takahide Nishi and Shojiro Miyazaki and Toshiyasu Takemoto and Keisuke Suzuki and Yukiko Iio and Katsuyoshi Nakajima and Takashi Ohnuki and Yumi Kawase and Futoshi Nara and Shinichi Inaba and Takashi Izumi and Hiroshi Yuita and Keiko Oshima and Hiromi Doi and Ryotaku Inoue and Wataru Tomisato and Takashi Kagari and Takaichi Shimozato},
  journal={ACS medicinal chemistry letters},
  volume={2 5},
CS-0777 (3) is phosphorylated in vivo, and the phosphate of CS-0777 (CS-0777-P) (4) acts as a selective S1P receptor-1 (S1P1) modulator. We report herein the synthesis of CS-0777 and CS-0777-P, pharmacological effects such as S1P1 and S1P3 agonist activity in vitro, peripheral blood lymphocyte lowering effects and the suppressive effect on experimental autoimmune encephalomyelitis (EAE), and also the pharmacokinetics in rats. CS-0777-P had ∼320-fold greater agonist activity for human S1P1 (EC50… CONTINUE READING


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