1306760-73-5
1306760-73-5 structure
- Name: RP101075
- Chemical Name: Benzonitrile, 5-[3-[(1S)-1-amino-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)-
- CAS Number: 1306760-73-5
- Molecular Formula: C21H20N4O2
- Molecular Weight: 360.4091
- Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
- Create Date: 2018-07-20 03:48:33
- Modify Date: 2024-01-16 15:58:02
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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].
| Name | Benzonitrile, 5-[3-[(1S)-1-amino-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-methylethoxy)- |
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| Description | 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]. |
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| Related Catalog | |
| Target |
S1PR1:0.27 nM (EC50) S1PR5:5.9 nM (EC50) |
| 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). |
| References |
| Molecular Formula | C21H20N4O2 |
|---|---|
| Molecular Weight | 360.4091 |