Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 2,570.00 | |
50 mg | 10-14 weeks | $ 3,380.00 | |
100 mg | 10-14 weeks | $ 4,600.00 |
Description | A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis. |
Targets&IC50 | RORβ:1370 nM , RORγt:5 nM , RORα:73 nM |
In vitro | A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50s: 38 nM, 20 nM, 25 nM and 64 nM). 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). 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. |
Molecular Weight | 527.36 |
Formula | C25H23Cl2F3N2O3 |
CAS No. | 2055271-22-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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A-9758 2055271-22-0 Metabolism ROR A9758 A 9758 inhibitor inhibit