产品
编 号：F677987
分子式：C21H20N4O2
分子量：360.41
分子式：C21H20N4O2
分子量：360.41
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CAS No: 1306760-73-5
产品详情
生物活性：
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.
体内研究：
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.RP101075 (0.3-3 mg/kg; p.o.; daily from week 23 until week 42) inhibits lymphocytes and pDC in the spleens of mice.Animal Model:NZBWF1 female mice
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).
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.
体内研究：
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.RP101075 (0.3-3 mg/kg; p.o.; daily from week 23 until week 42) inhibits lymphocytes and pDC in the spleens of mice.Animal Model:NZBWF1 female mice
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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