rorγt

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.

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

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.

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

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

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 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 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 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.

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

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

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 Inverse Agonist 3 is a potent, selective, and orally active inverse agonist of RORγ with EC50 values of 0.22 μM for hRORγ and 0.15 μM for RORγt (human IL-17 cells), respectively.

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].

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.

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

Cedirogant (ABBV-157) is an orally active, retinoid-related orphan receptor-γt (RORγt) inverse agonist used in psoriasis studies.

Bevurogant is an antagonist of RORγt receptor and can be used in studies about the treatment of chronic inflammatory diseases.

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

TMP920 inhibits RORγt binding to the SRC1 peptide (IC50: 0.03 μM). TMP920 is a highly potent and selective RORγt antagonist.

SR0987 is a RORγt agonist,

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

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

GSK805 is a potent, orally bioavailable and CNS-penetrant RORγt inhibitor.

TMP-778 is a selective inverse agonist of RORγt.

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 1.9 nM and a reporter gene IC50 of 6.1 nM.

BMS-986313 is a RORγt Inverse Agonist with RORγt EC50 = 3.6 nM and WB EC50 = 50 nM.

FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells. FM26 is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM.

MRL-871 (compound 3) is a potent inverse agonist of the isotretinoin receptor-related orphan receptor γt (RORγt) with an IC50 of 264 nM. Possessing a specific isoxazole chemotype, MRL-871 effectively reduces IL-17a mRNA production in EL4 cells.

BIO399 is an agonist of the RORγt inverse.

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

TMP780 is an inverse RORγt agonist (IC50: 13 nM). RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

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.

JNJ-61803534 is a potent, orally active RORγt inverse agonist, demonstrating anti-inflammatory activity through inhibition of IL-17A production in human CD4+ T cells under Th17 differentiation conditions, with an IC50 of 9.6 nM.

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.

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 .