1. Metabolic Enzyme/Protease
    Immunology/Inflammation
  2. ROR
    Interleukin Related
  3. A-9758

A-9758 

Cat. No.: HY-126252
Handling Instructions

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.

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

A-9758 Chemical Structure

A-9758 Chemical Structure

CAS No. : 2055271-22-0

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Description

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[1].

IC50 & Target

IC50: 5 nM (RORγt), 73 nM (RORα), 1370 nM (RORβ)[1]

In Vitro

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].

Molecular Weight

527.36

Formula

C₂₅H₂₃Cl₂F₃N₂O₃

CAS No.

2055271-22-0

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

Shipping

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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A-9758
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HY-126252
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