rorγ

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist (IC50=63.8 nM), with improved drug-like properties[1].

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

RORγ antagonist 1 (compound 22), a potent derivative of betulinic acid, acts as an antagonist to RORγ with a dissociation constant (K D) of 0.18 μM. It demonstrates anti-proliferative effects in the HPAF-II pancreatic cancer xenograft model, inhibits the RAS/MAPK and AKT/mTORC1 signaling pathways, and triggers caspase-dependent apoptosis in pancreatic cancer cells [1].

RORγt modulator 5, a potent RORγt modulator, exhibits a dissociation constant (K_i) of <100 nM. This compound holds promise for the treatment of diseases mediated by RORγ, including inflammatory, metabolic, and autoimmune disorders.

RORγ agonist 1 is a highly potent and orally bioavailable compound that activates the RORγ receptor. Its efficacy is demonstrated by an EC50 value of 21 nM and it exhibits antitumor activity.

RORγt inverse agonist 31 (14g) is a potent antagonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an inhibitory concentration (IC50) of 0.428 μM. It has demonstrated efficacy in mitigating Imiquimod-induced psoriasis severity in murine models [1].

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist (IC50: 46 nM). Targeting the nuclear receptor RORγt is effective in the treatment of autoimmune diseases.

RORγt/DHODH-IN-3 (compound (S)-14d) is a potent, orally active dual inhibitor of RORγt (IC50: 0.098 μM) and DHODH (IC50: 0.432 μM).RORγt/DHODH-IN-1 has significant in vivo anti-inflammatory effects.

RORγt/DHODH-IN-1 (compound (R)-14d) is a potent, orally active dual inhibitor of RORγt (IC50: 0.083 μM) and DHODH (IC50: 0.172 μM), which exhibits significant in vivo anti-inflammatory effects.

RORγt inverse agonist 28 is a potent RORγt inverse agonist. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has shown research potential in inflammatory and autoimmune diseases.

RORγt inverse agonist 23, an orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist, is a potent and selective RORγt inverse agonist.

RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines and thus enhances lymphocyte cytotoxicity. rorγt agonist 2 exhibits an inhibitory effect on the production of regulatory T cells and is able to suppress immune responses.

RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines and thus increases lymphocyte cytotoxicity. rorγt agonist 3 blocks the production of regulatory T cells and suppresses the immune response.

RORγt inverse agonist 29 is a potent, selective, orally active RORγt inverse agonist with an IC50 value of 21 nM. RORγt inverse agonist 29 can be used in the study of autoimmune diseases such as skin inflammation and psoriasis.

RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.

RORγt inverse agonist 26, a potent reverse agonist of RORγt, effectively modulates Th17 cell differentiation and suppresses IL-17 production. This compound shows promising potential for researching inflammation and autoimmune diseases.

RORγt modulator 2 is a modulator of retinol-related orphan receptor γt (RORyt) (IC50<50 nM) and can be used in the study of RORγt-mediated diseases such as pain, inflammation, asthma, rheumatoid arthritis, COPD, multiple sclerosis, psoriasis, colitis, neurodegenerative diseases and cancer.

RORγt modulator 4 is a RORγt modulator that regulates IL-17A production activity in cells derived from mouse spleen.

RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor that can be used in the study of inflammatory bowel disease (IBD).

RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.

RORγt inverse agonist 14 (8e) is a potent, selective, and orally active compound with an EC50 of 2.5 nM, exhibiting anti-inflammatory activity. It is employed in researching rheumatoid arthritis and psoriasis [1].

RORγt Inhibitor 2, a potent inhibitor of RORγt, exhibits an IC50 of 9.2 nM and is utilized in the study of cancer, inflammation, or autoimmune diseases that are mediated by RORγt.

RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC 50 value of 1 nM.

RORγt modulator 3 is a modulator of retinol-related orphan receptor γt (RORγt) and can be used to study RORγt-mediated diseases such as pain, COPD, inflammation, asthma, colitis, multiple sclerosis, rheumatoid arthritis, psoriasis, neurodegenerative diseases and cancer.

ROR Modulator I is the first potent inverse agonist of the retinoid-related orphan receptor. It also has dual selectivity for RORβ and RORγt.

ROR agonist-1 is a potent and orally bioavailable the retinoic acid receptor-related orphan receptor C2 (RORC2) inverse agonist(inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5).

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

RORγt Inverse agonist 3 is a potent, selective and orally active inverse agonist of RORγ(EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively).

RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM).

RORγt Inverse agonist 2 is a selective, orally active inverse agonist of RORγt(EC50 of 119 nM).

RORγt agonist 1 is a potent, orally bioavailable agonist of RORγt(EC50 of 20.8 nM).

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor κB (NF κB).

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α γ.

BIO592 is a modulator of RORγt. BIO592 triggers inverse agonism of RORγ.

ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r

XY 018 is a RORγ antagonist. It also suppresses androgen receptor expression in prostate cancer cell lines and inhibits the growth of tumors in androgen receptor-positive xenograft models.

GNE-0946 is a potent and selective agonist of RORγ (EC50: 4 nM for HEK-293 cell).

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

JTE-151 is a novel RORγ inverse agonist.

GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 possessed favorable RORc cellular potency with 75-fold selectivity for RORc over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors in a cell assay panel. The favorable potency, selectivity, in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in a PK/PD model support the evaluation of GNE3500 in preclinical studies (J. Med. Chem., 2015, 58 (13), pp 5308–5322)

Retezorogant is a retinoic acid receptor-related orphan receptor gamma (RORγ) antagonist.

CD12681 is an effective RORγ inverse agonist, preclinical Candidate for the topical therapy of psoriasis.

Cintirorgon (LYC-55716) is a selective, oral agonist of RORγ. Cintirorgon modulates gene expression of RORγ expressing T lymphocyte immune cells.

7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated human na ve CD4+ T cells when used at a concentration of 300 nM. 7β,27-dihydroxy Cholesterol (60 mg/kg) increases IL-17A production in isolated mouse γδ T cells stimulated with 12-myristate 13-acetate and ionomycin .

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

SR 1555 is a novel RORγ-specific synthetic ligand.

SR 1001 is an inverse agonist for RORα/RORγ (Kis: 172/111 nM).