rorα

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

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

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

RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with an IC50 of 46 nM, making it effective in the treatment of autoimmune diseases by targeting the nuclear receptor RORγt.

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) with significant in vivo anti-inflammatory effects.

RORγt agonist 4 (compound 14) acts as a potent and selective agonist for RORγt, significantly boosting metabolic stability. It also enhances the condition in mouse tumor models, specifically B16F10 melanoma and LLC lung adenocarcinoma [1].

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

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), exhibiting significant in vivo anti-inflammatory effects.

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

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

RORγt Inverse agonist 10 is a highly potent, 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 RORγt activity, a key transcription factor regulating genes linked to psoriasis pathogenesis, including [IL-17A], [IL-22], and [IL-23R].

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 that induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines, and enhances lymphocyte cytotoxicity. It exhibits an inhibitory effect on the production of regulatory T cells and can suppress immune responses.

RORγt agonist 3 is a potent agonist of RORγt that induces Th17 cell differentiation, increases levels of pro-inflammatory cytokines, and enhances lymphocyte cytotoxicity. Moreover, [it] blocks the production of regulatory T cells and suppresses the immune response.

RORγt inverse agonist 29 is a potent, selective, and orally active compound with an IC50 value of 21 nM. It can be utilized in the study of autoimmune diseases, including skin inflammation 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 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 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.

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 in mouse spleen-derived cells.

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 DHODH-IN-2 (compound 1) is a potent dual inhibitor of RORγt and DHODH, useful for studying inflammatory bowel disease (IBD).

ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), demonstrating inhibition of IL-17A production from human primary TH17 cells with a pIC50 of 7.5.

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 an RORγt allosteric inhibitor with an IC50 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.

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

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.

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.

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.

Vimirogant (VTP-43742) hydrochloride is an orally active, selective RORγt inhibitor (IC50: 17 nM, Ki: 3.5 nM) that is more than 1000 times more selective than RORα and RORβ. It inhibits Th17 differentiation and IL-17A secretion in mouse spleen cells with an IC50 of 57 nM and does not affect Th1, Th2, or Treg cell differentiation.

A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.

1. Neoruscogenin represents a universal pharmacological tool for RORα research due to its specific selectivity profile versus other nuclear receptors.

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

BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE). 5J-4 reduces the production of IL-17 and decreases the expression of RORα and RORγt.

SR3335 (ML 176) is a selective inverse agonist of RORα that competitively inhibits the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).