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A-9758

  Cat. No.:  DC70164  
Chemical Structure
2055271-22-0
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More than 5000 active chemicals with high quality for research!
Field of application
A-9758 (A9758) is a selective, small molecule inverse agonist of retinoid-related orphan receptor gamma t (hRORγt IC50=38 nM).A-9758 also inhibits mouse RORγ transactivation with similar activity (20 nM) and is equally active on dog and rat RORγ (25 and 64 nM, repectively).A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM in human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively.A-9758 exhibits robust potency against IL-17A release both in vitro and in vivo, significantly attenuates IL-23 driven psoriasiform dermatitis.A-9758 exhibits efficacy in an ex vivo human whole blood assay, is efficacious in human IL-17 related diseases.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2055271-22-0
Chemical Name: A-9758
Synonyms: A9758, A 9758
Formula: C25H23Cl2F3N2O3
M.Wt: 527.365
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC73863 ODH-08 ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice. ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs). ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β.
DC47003 Bevurogant Bevurogant is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.
DC46880 Cedirogant Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.
DC44172 RORγt inverse agonist 13 RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.
DC44171 RORγt Inverse agonist 6 RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
DC11846 TMP778 TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.
DC11046 SR2211 SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells.
DC11047 MRL871 MRL-871 (MRL871) is a potent, selective inhibitor of RORγt via allosteric inverse agonism, inhibits coactivator binding with IC50 of 7 nM; significantly reduces the IL17a mRNA levels in EL4 murine lymphoblast cell line at 10 uM.
DC73865 W6134 W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.
DC73864 PCCR-1 PCCR-1 is a potent, specific RORγ inhibitor with binding IC50 of 34.45 nM and 778.1 nM for human and mouse RORγ, respectively, > 300-fold selectivity over other isoforms of ROR.
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