RWT9996
RWT9996 is a GPR17 antagonist. RWT9996 inhibits GPR17-mediated signal transduction processes, including G protein activation and β-arrestin-2 recruitment. RWT9996 inhibits MDL-29951 (HY-16312)-mediated phosphorylation of ERK1/2, phosphorylation of CREB, and accumulation of inositol phosphate (IP1) in oligodendrocyte precursor cells in vitro. RWT9996 can be used in studies related to demyelinating diseases.
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- CAS. Nr.: 2877694-62-5
- Formel: C17H12FN3O2S
- Molecular Weight:341.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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ERK1 |
ERK2 |
Arrestin-3/β-Arrestin 2 |
RWT9996 (12 min) potently inhibits MDL-29951-mediated activation of Gαi2, Gαz and Gα12 in FlpIn-HEK293-hGPR17S cells, with pKB values ranging from 7.7 to 8.3, but induces non-specific effects[1].
RWT9996 potently inhibits MDL-29951-mediated recruitment of β-arrestin-2 to GPR17 in HEK293T cells[1].
RWT9996 (pre-incubated for 10 min, stimulated for 2 min) potently inhibits ERK1/2 phosphorylation in differentiated Oli-neu cells with a pIC50 value of 8.2; it potently inhibits the first phase of CREB phosphorylation induced by MDL-29951 (HY-16312) with a pIC50 of 8.1; and it inhibits IP1 accumulation with a pIC50 of 7.0, where this accumulation is slightly enhanced by Barbadin (HY-119706)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2877694-62-5
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Molecular Weight 341.36
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Formel C17H12FN3O2S
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SMILES
FC1=C(NS(C2=CNC(C3=CC=CC=C3)=C2)(=O)=O)C=CC(C#N)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)