| Identification | Back Directory | [Name]
Benzonitrile, 5-[3-[(1S)-1-amino-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)- | [CAS]
1306760-73-5 | [Synonyms]
RP-101075
Ozanimod Impurity 7
Benzonitrile, 5-[3-[(1S)-1-amino-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)- | [Molecular Formula]
C21H20N4O2 | [MOL File]
1306760-73-5.mol | [Molecular Weight]
360.41 |
| Hazard Information | Back Directory | [Uses]
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile[1]. | [in vivo]
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).
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| [IC 50]
S1PR1: 0.27 nM (EC50); S1PR5: 5.9 nM (EC50) | [References]
[1] Sun N, et al. Selective Sphingosine-1-Phosphate Receptor 1 Modulation Attenuates Experimental Intracerebral Hemorrhage. Stroke. 2016;47(7):1899-1906. DOI:10.1161/STROKEAHA.115.012236
[2] Taylor Meadows KR, et al. Ozanimod (RPC1063), a selective S1PR1 and S1PR5 modulator, reduces chronic inflammation and alleviates kidney pathology in murine systemic lupus erythematosus. PLoS One. 2018;13(4):e0193236. Published 2018 Apr 2. DOI:10.1371/journal.pone.0193236 |
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