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

RP101075 

Cat. No.: HY-136576
Handling Instructions

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.

For research use only. We do not sell to patients.

RP101075 Chemical Structure

RP101075 Chemical Structure

CAS No. : 1306760-73-5

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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].

IC50 & Target[1]

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).
Molecular Weight

360.41

Formula

C₂₁H₂₀N₄O₂

CAS No.

1306760-73-5

SMILES

N#CC1=CC(C2=NC(C3=CC=CC4=C3CC[[email protected]@H]4N)=NO2)=CC=C1OC(C)C

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

RP101075RP 101075RP-101075LPL ReceptorDrug MetaboliteLysophospholipid Receptorchronic,inflammationcardiovascularcelldeathmetabolitelymphocytesneutrophilsInhibitorinhibitorinhibit

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RP101075
Cat. No.:
HY-136576
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