PIPE-3297
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity.
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- Formule: C23H30N2O
- Masse moléculaire:350.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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κ Opioid Receptor/KOR 1.1 nM (EC50) |
In Vitro
PIPE-3297 induces myelination and causes oligodendrocyte progenitor cells (OPCs) differentiation into oligodendrocytes (OLs)[1].
PIPE-3297 exhibits cardiotoxity with 72% hERG inhibition (3 μM) and unstability in liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OPC
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Concentration:0.5-1 μM
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Incubation Time:72 h
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Result:Increased levels of MBPs
In Vivo
PIPE-3297 (30 mg/kg, s.c., single dosage) induces KOR-dependent OPC differentiation into mature OLs in C57BL/6 mice[1].
PIPE-3297 (3 and 30 mg/kg, s.c., daily for 23 days) ameliorates the autoimmune encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG) in C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOG induced EAE in C57BL/6 mice[1]
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Dosage:3 and 30 mg/kg
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Administration:s.c., daily for 23 days
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Result:Ameliorated the EAE.
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Animal Model:C57BL/6 mice[1]
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Dosage:3 and 30 mg/kg
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Administration:s.c., single dose
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Result:Increased levels of KOR and mature OLs, maintained the locomotion ability.
Chemical Information
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Masse moléculaire 350.50
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Formule C23H30N2O
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SMILES
OC1=CC=CC(CCN(C2CN(C2)CC3=CC=CC=C3)CC4CCC4)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PIPE-3297 Related Classifications
HY-163277 Related Classifications
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