RP101442 是 Ozanimod 的主要的活性代谢物，是一种选择性强的 S1PR1 激动剂，对 S1PR1 和 S1P5R 的 EC50 分别为 0.19 nM 和 32.8 nM。
货号:ajcx39358
CAS:N/A
分子式:C23H22N4O4
分子量：418.45
溶解度:DMSO : 125 mg/mL (298.72 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

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)