RP101075
Modify Date: 2024-01-16 15:58:02
RP101075 structure
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Common Name | RP101075 | ||
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| CAS Number | 1306760-73-5 | Molecular Weight | 360.4091 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H20N4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RP101075RP101075, 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 |
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| Molecular Weight | 360.4091 |