A-9758
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
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- CAS No.: 2055271-22-0
- Formule: C25H23Cl2F3N2O3
- Masse moléculaire:527.36
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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
Activité biologique
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RORγt 5 nM (IC50) |
IL-17A |
IL-23 |
A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50=38 nM, 20 nM, 25 nM and 64 nM, respectively)[1].
A-9758 displays a cofactor profile in recruiting co-repressors (NCoR1: EC50=60 nM, NCoR2: EC50=43 nM) and derecruiting co-activators (NCoA1: IC50=110 nM, PGC1α: IC50=49 nM)[1].
A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM for human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively. A-9758 attenuates the differentiation of RORγt expressing Th17 cells and/or their effector function[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2055271-22-0
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Masse moléculaire 527.36
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Formule C25H23Cl2F3N2O3
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SMILES
O=C(C1CCN(C(C2=CC=C(Cl)C(CC(N3C)=CC4=C3C=C(C(F)(F)F)C=C4C)=C2Cl)=O)CC1)O
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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)
A-9758 Related Classifications
HY-126252 Related Classifications
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