2. GPCR/G Protein Metabolic Enzyme/Protease
  3. LPL Receptor Drug Metabolite
  4. RP101075

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。

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RP101075 Chemical Structure

RP101075 Chemical Structure

CAS No. : 1306760-73-5

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RP101075 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 LPL Receptor 亚型特异性产品:

查看所有亚型
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

RP101075 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RP1010751306760-73-5RP 101075RP-101075LPL ReceptorDrug MetaboliteLysophospholipid Receptorchronic,inflammationcardiovascularcelldeathmetabolitelymphocytesneutrophilsInhibitorinhibitorinhibit

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产品名称：
RP101075
目录号：
HY-136576
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