规格: | 98% |
分子量: | 418.45 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Background:
RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely[1].
RP101988 is a substrate of P-gp and breast cancer resistance protein (BCRP) drug transporters[2].
[1]. Tran JQ, et al. Cardiac Safety of Ozanimod, a Novel Sphingosine-1-Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study. Clin Pharmacol Drug Dev. 2018;7(3):263-276.
[2]. Gilardi D, et al. PK, PD, and interactions: the new scenario with JAK inhibitors and S1P receptor modulators, two classes of small molecule drugs, in IBD [published online ahead of print, 2020 Jul 1]. Expert Rev Gastroenterol Hepatol. 2020;1-10.
Protocol:
S1PR1 0.19nM(EC50) | S1PR5 32.8nM(EC50) |