RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC 50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC 50 =5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile.

RP101075 (0.3-0.6 mg/kg; p.o.) significantly attenuated neurological deficits and reduced brain edema in intracerebral hemorrhage (ICH) mice. RP101075 reduced the counts of brain-infiltrating lymphocytes, neutrophils, and microglia, as well as cytokine expression after ICH. Enhanced blood-brain barrier integrity and alleviated neuronal death were also seen in ICH mice after RP101075 treatment[1]. RP101075 (0.3-3 mg/kg; p.o.; daily from week 23 until week 42) inhibits lymphocytes and pDC in the spleens of mice[2]. Animal Model: NZBWF1 female mice[2]Dosage: 0.3, 1, 3 mg/kg Administration: P.o.; daily from week 23 until week 42 Result: Dose-dependent reduction in lymphocytes in the spleen following 20 weeks of treatment; a reduction in plasmacytoid dendritic cells (pDC).

1306760-73-5

C21H20N4O2

360.41

RP101075

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years