RORγ Inhibitor

Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease.

BMS-336 (Compound 89) is a RORγ inhibitor. BMS-336 can be used for the research of cancer.

SPH7854 is a RORγt inhibitor with human RORγt IC₅₀ of 10 nM, high selectivity over RORα and RORβ, and oral effectiveness. SPH7854 suppresses RORγt activity, Th17 cell differentiation, and IL-17 production. SPH7854 can be used for the research of inflammatory bowel disease.

Izumerogant (IMU-935) is an orally active RORγ/DHODH dual inhibitor with IC₅₀s of 10 and 98 nM against RORγ and DHODH. Izumerogant efficiently blocks the replication of SARS-CoV-2, HCMV and HAdV5 with EC₅₀ values between 3.6 and 17 nM. Izumerogant can be used for researching antiviral properties.

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

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

Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (K_i=3.5 nM; IC₅₀=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC₅₀=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.

S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC₅₀ of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC₅₀>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations.

W6134 is highly potent and selective RORγ covalent inhibitor with an IC₅₀ of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC).

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.

RORγt inhibitor 4 (Compound 9a) is an orally active and a CNS-penetrating RORγt inhibitor. RORγt inhibitor 4 improves experimental autoimmune encephalomyelitis.

RORγt inverse agonist 33 (compound (R)-D4) is an orally bioavailable and inverse agonists of RORγt, with the IC₅₀ of 21 nM. RORγt inverse agonist 33 plays an important role in rheumatoid arthritis research.

RORγ-IN-3 (Compound 21) is a potent and highly selective RORγ inhibitor with an EC₅₀ of 84 nM. RORγ-IN-3 can effectively inhibit the production of IL-17, with an IC₅₀ value of 1.0 μM. RORγ-IN-3 can be used for the study of autoimmune diseases.

RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC₅₀ of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research.

RORγt inverse agonist 32 (compound b14) is orally active. RORγt inverse agonist 32 can be used in inflammation research.

RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC₅₀: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis.

RORγ-IN-2 (Compound 22) is a RORγ inhibitor, with a K_i of 16.6 nM for hRORγ. RORγ-IN-2 can be used for the research of IL-17-dependent autoimmune diseases.

RORγt inverse agonist 36 (S configuration of Compound 16) is a RORγt inverse agonist. RORγt inverse agonist 36 can be used for the research of inflammation and immunology.

RORγ-IN-4 is a RORγ inhibitor with an EC₅₀ of 0.014 μM. RORγ-IN-4 can be used for the research of inflammation.

CID 7309015 is an inhibitor of retinoic acid-related orphan receptor gamma (ROR-γ). CID 7309015 can be used for research of inflammation, NF-κB signaling or inflammatory arthritis.