Uses
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS)[1].
References
[1] Takahide Nishi *?, Shojiro Miyazaki ?, Toshiyasu Takemoto ?, Keisuke Suzuki ?, Yukiko Iio ?, Katsuyoshi Nakajima ?, Takashi Ohnuki ?, Yumi Kawase ?, Futoshi Nara ?, Shinichi Inaba §, Takashi Izumi §, Hiroshi Yuita , Keiko Oshima , Hiromi Doi , Ryotaku Inoue , Wataru Tomisato , Takashi Kagari , and Takaichi Shimozato * .Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist
ACS Med. Chem. Lett., 2011, 2 (5), pp 368-372
DOI: 10.1021/ml100301k
Publication Date (Web): March 2, 2011
