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.
Product information
CAS Number: 2055271-22-0
Molecular Weight: 527.36
Formula: C25H23Cl2F3N2O3
Chemical Name: 1-(2,4-dichloro-3-{[1,4-dimethyl-6-(trifluoromethyl)-1H-indol-2-yl]methyl}benzoyl)piperidine-4-carboxylic acid
Smiles: CN1C2=CC(=CC(C)=C2C=C1CC1C(Cl)=CC=C(C=1Cl)C(=O)N1CCC(CC1)C(O)=O)C(F)(F)F
InChiKey: NVDKGFYFKVWJLJ-UHFFFAOYSA-N
InChi: InChI=1S/C25H23Cl2F3N2O3/c1-13-9-15(25(28,29)30)10-21-18(13)11-16(31(21)2)12-19-20(26)4-3-17(22(19)27)23(33)32-7-5-14(6-8-32)24(34)35/h3-4,9-11,14H,5-8,12H2,1-2H3,(H,34,35)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50=38 nM, 20 nM, 25 nM and 64 nM, respectively). 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.
Products are for research use only. Not for human use.
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