Bioactivity | 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]. | ||||||||||||
Invitro | RP101988 is a substrate of P-gp and breast cancer resistance protein (BCRP) drug transporters[2]. | ||||||||||||
Name | RP101988 | ||||||||||||
Formula | C23H22N4O4 | ||||||||||||
Molar Mass | 418.45 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |