RP101075

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RP101075

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1306760-73-5

RP101075 是 Ozanimod 的活性代谢物，是一种有效的口服S1PR1激动剂，EC₅₀为 0.27 nM。RP101075 在 S1PR5 (EC₅₀=5.9 nM) 上的选择性大于 100 倍，在 S1PR 2、3 和 4 上的选择性大于 10000 倍。RP101075 显示优越的心血管安全性。

生物活性

RP101075, an active metabolite of Ozanimod, is a potent, orally activeS1PR(sphingosine-1-phosphate receptor 1) agonist, with anEC₅₀of 0.27 nM. RP101075 displays >100-fold selectivity overS1PR5(EC₅₀=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile^[1].

IC₅₀& Target^[1]

S1PR1

0.27 nM (EC₅₀)

S1PR5

5.9 nM (EC₅₀)

体内研究
(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).

分子量

360.41

Formula

C₂₁H₂₀N₄O₂

CAS 号

1306760-73-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.