Catalog No.
Product Name
Application
Product Information
Citations
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RORγ modulator
RORγ modulator 1 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124. -
RORγ agonist
LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist. -
RORγt inhibitor
AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis. -
FAA1 agonist
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. -
ROR agonist
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5. -
RORγt inhibitor
S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production. -
RORγt inverse agonist
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity. -
RORγt inverse agonist
(Rac)-TMP778 is the racemate of TMP778. TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay. -
RORγt inverse agonist
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM. -
ROR gamma modulator
Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2. -
RORγ Inhibitor
W6134 is a potent and selective covalent inhibitor of RORγ, displaying an IC50 of 0.21 μM. This compound demonstrates remarkable selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 effectively suppresses RORγ transcriptional activity and has been shown to inhibit proliferation and colony formation while inducing apoptosis in castration-resistant prostate cancer (CRPC) cells. It is a valuable tool for investigating the mechanisms and treatment strategies for CRPC. -
RORγt Inverse Agonist
BMS-986251 is a selective RORγt inverse agonist with an EC50 of 12 nM in RORγt GAL4 assays. It effectively inhibits IL-17 production with an EC50 of 24 nM in human whole blood assays. BMS-986251 exhibits significant efficacy in preclinical models of psoriasis, including mouse acanthosis and Imiquimod-induced models, making it a valuable tool for research in autoimmune and inflammatory diseases. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-1 is a dual inhibitor targeting RORγ and dihydroorotate dehydrogenase (DHODH) with IC50 values of 9.7 nM and 100 nM, respectively. This compound effectively inhibits the replication of SARS-CoV-2, human cytomegalovirus (HCMV), and adenovirus type 5 (HAdV5), making it a valuable tool in viral research. Its dual mechanism of action allows for potential applications in understanding viral-pathogen interactions and developing therapeutic strategies against viral infections. -
ROR2 ADC
Ozuriftamab vedotin is an antibody-drug conjugate (ADC) targeting the receptor tyrosine kinase orphan receptor 2 (ROR2). This compound combines a humanized monoclonal antibody, Ozuriftamab, with the cytotoxic agent VcMMAE, enabling selective delivery to ROR2-expressing tumor cells. Ozuriftamab vedotin exhibits potent antitumor activity and is utilized in research focused on cancer therapeutics and targeted therapies. -
ROR1 ADC Intermediate
BL20-MMAE is an antibody-drug conjugate designed to target the receptor tyrosine kinase ROR1. This compound is synthesized by linking an anti-ROR1 antibody with the cytotoxic agent MMAE through a BL20 linker, facilitating targeted delivery of the drug. BL20-MMAE is primarily utilized in research applications focused on cancer therapeutics, particularly in studies involving ROR1-positive malignancies. -
RORγ Inverse Agonist
SR-1903 is an inverse agonist of RORγ and PPARγ, exhibiting IC50 values of approximately 100 nM and 209 nM for these targets, respectively. This compound demonstrates significant anti-inflammatory and anti-diabetic properties, making it valuable in models of collagen-induced arthritis and diet-induced obesity. SR-1903's unique mechanism of action positions it as a useful reagent in researching metabolic disorders and inflammatory diseases. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-2 is a potent dual inhibitor of RORγ and DHODH, exhibiting IC50 values of 11.9 nM and 90 nM, respectively. This compound demonstrates significant antiviral activity against multiple viruses, including SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively. RORγ/DHODH-IN-2 is ideal for research applications targeting immune signaling pathways and viral infections. -
RORγ/DHODH Inhibitor
Izumerogant (IMU-935) is an orally active dual inhibitor of RORγ and DHODH, with IC50 values of 10 nM and 98 nM, respectively. This compound effectively disrupts the replication of various viruses, including SARS-CoV-2, HCMV, and HAdV5, demonstrated by EC50 values ranging from 3.6 to 17 nM. Izumerogant serves as a valuable tool for investigating antiviral mechanisms and therapeutic strategies against viral infections. -
RZR/ROR Receptor Agonists
CGP52608 is a selective agonist for the RZR/ROR receptor, exhibiting notable anti-tumor activity with minimal interaction with the cell surface G-protein coupled melatonin receptor. This compound has been demonstrated to inhibit the proliferation of mouse 16/C breast cancer cells, making it a valuable tool in cancer research. Additionally, CGP52608 is effective in inducing vesicle formation in diatoms, providing insights into cellular mechanisms and developmental processes. -
GPBAR1 Agonist/RORγt Inhibitor
Allolithocholic acid functions as a dual agonist of GPBAR1 and an inverse agonist of RORγt, exhibiting an EC50 of 2.7 μM and an IC50 of 3.4 μM, respectively. This compound modulates immune and metabolic pathways by influencing immune cell polarization and preventing the differentiation of M1 macrophages and Th17 CD4 cells. Allolithocholic acid enhances insulin sensitivity and mitigates liver lipid accumulation, while also restoring bile acid homeostasis and modulating intestinal immunity. It is a valuable reagent for research in cancer, inflammation, immunology, and metabolic disorders. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-1 is a dual inhibitor targeting retinoic acid receptor-related orphan receptor gamma t (RORγt) and dihydroorotate dehydrogenase (DHODH). With IC50 values of 0.083 μM for RORγt and 0.172 μM for DHODH, this compound demonstrates significant potency. RORγt/DHODH-IN-1 has been shown to possess notable in vivo anti-inflammatory activity, making it a valuable tool for research in immunology and inflammation-related studies. -
Dual RORγt/DHODH Inhibitor
RORγt/DHODH-IN-3 is a dual inhibitor targeting both RORγt and dihydroorotate dehydrogenase (DHODH), exhibiting IC50 values of 0.098 μM for RORγt and 0.432 μM for DHODH. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for researchers investigating autoimmune diseases and other inflammatory conditions. Its dual mechanism of action positions it as a promising candidate for therapeutic development in these areas. -
RORγt/DHODH Inhibitor
RORγt/DHODH-IN-2 is a potent dual inhibitor of RORγt and DHODH, targeting key pathways involved in immune regulation and inflammation. This compound exhibits significant biological activity that can be leveraged in the investigation of inflammatory bowel disease (IBD) and related immune disorders. Its dual action provides a valuable tool for research into therapeutic strategies aimed at modulating RORγt and DHODH activity in inflammatory contexts. -
RORγ Agonist
Zymostenol (5a-Cholest-8-en-3b-ol) is a RORγ agonist with an EC50 of 1 μM. This compound plays a significant role as a late-stage precursor in cholesterol biosynthesis, facilitating the modulation of immune responses. Zymostenol is primarily utilized in research applications focused on investigating the mechanisms of RORγ signaling and its implications in various biological processes and diseases. -
RORγt Inhibitor
RORγt inverse agonist 36 is a selective inverse agonist targeting the retinoid-related orphan receptor gamma t (RORγt). This compound modulates RORγt activity, leading to inhibition of Th17 cell differentiation and cytokine production. It is primarily utilized in research focused on inflammation and immunology, offering valuable insights into therapeutic approaches for autoimmune diseases. -
RORγt Inverse Agonist
RORγt Inverse Agonist 30 is a selective inverse agonist of the RORγt nuclear receptor, exhibiting an IC50 of 46 nM. This compound effectively modulates RORγt activity, making it a valuable tool in the study of autoimmune disorders. Its ability to inhibit RORγt function positions it as a promising candidate for research into therapeutic strategies for conditions such as multiple sclerosis and other inflammatory diseases. -
RORC modulator
RORC modulator-1 is a selective modulator of the retinoic acid receptor-related orphan receptor C (RORC). It demonstrates the ability to regulate RORC activity, impacting the expression of genes involved in immune response and inflammation. This compound is valuable for research applications focused on T helper cell differentiation, autoimmune diseases, and the study of related signaling pathways. -
ROR-γ Inhibitor
CID 7309015 is a selective inhibitor of retinoic acid-related orphan receptor gamma (ROR-γ). This compound demonstrates significant potential in modulating inflammatory pathways, particularly in the context of NF-κB signaling and inflammatory arthritis research. CID 7309015 serves as a valuable tool for investigating the roles of ROR-γ in immune response and inflammatory diseases. -
RORγt Inhibitor
RORγt inhibitor 3 is a potent and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), which plays a crucial role in Th17 cell differentiation. This compound demonstrates high binding affinity and effectively modulates immune responses, making it particularly relevant for research in autoimmune disorders. Its efficacy has been validated in mouse models of experimental autoimmune encephalomyelitis (EAE) and collagen-induced arthritis (CIA), highlighting its potential for therapeutic applications in inflammatory diseases. -
RORγ Agonist
Cintirorgon sodium is a selective and orally bioavailable RORγ agonist that modulates gene expression in RORγ-expressing T lymphocytes. This compound enhances effector functions and reduces immunosuppressive mechanisms, contributing to decreased tumor growth and improved survival rates in various preclinical models. Cintirorgon sodium is a valuable tool for research applications focused on immunotherapy and cancer biology. -
TH17 Cell Differentiation Inhibitor
3-Oxo-5β-cholanoic acid, also known as Dehydrolithocholic acid, functions as a potent inhibitor of TH17 cell differentiation. This compound achieves its biological activity by directly binding to the transcription factor RORγt, with a dissociation constant (Kd) of 1.13 μM. It is useful in research applications aimed at understanding inflammatory responses and immune modulation. -
RORγt Inhibitor
GSK805 is an orally active RORγt inhibitor that effectively modulates immune responses. Its mechanism involves inhibiting RORγ and the differentiation of Th17 cells, demonstrating pIC50 values of 8.4 and >8.2, respectively. GSK805 further suppresses Th17 cell functionality, making it a valuable tool for investigating immune-related disorders and therapeutic approaches targeting RORγt in inflammatory conditions. -
RORα Agoinst
Neoruscogenin is a high-affinity agonist of the nuclear receptor RORα (NR1F1), exhibiting an EC50 of 0.11 µM. This compound plays a crucial role in modulating gene expression and is involved in various physiological processes, including circadian rhythm and metabolism. Neoruscogenin is applicable in research areas focusing on nuclear receptor signaling and the development of therapeutics targeting metabolic disorders. -
ROR-γ Antagonist
XY018 is a selective antagonist of ROR-γ (retinoic acid receptor-related orphan receptor gamma), designed to inhibit its constitutive activity. With an EC50 value of 190 nM in 293T cells, XY018 effectively disrupts ROR-γ signaling by binding to its hydrophobic ligand binding domain. This compound is valuable for research applications focused on autoimmune diseases, metabolic disorders, and inflammation by modulating ROR-γ activity. -
RORγt Antagonist
Bevurogant is a selective antagonist of the retinoid-related orphan receptor gamma t (RORγt), which plays a critical role in immune response and inflammation. This compound is primarily utilized in research focused on chronic inflammatory diseases, offering insights into therapeutic strategies for conditions such as autoimmune disorders. Its ability to modulate RORγt activity makes it a valuable tool in the study of immune regulation and potential treatment pathways. -
RORγt Inverse Agonist
MRL-871 is a potent allosteric inverse agonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an IC50 of 12.7 nM. This compound is characterized by its unique isoxazole chemotype and demonstrates significant efficacy in reducing IL-17a mRNA production in EL4 cells. MRL-871 is useful for research applications focused on immune response modulation and studying the role of RORγt in autoimmune diseases. -
RORγt Inverse Agonist
JNJ-61803534 is a potent RORγt inverse agonist, exhibiting an IC50 of 9.6 nM. This compound demonstrates significant anti-inflammatory activity by inhibiting the production of IL-17A in human CD4+ T cells during Th17 differentiation. JNJ-61803534 is valuable for research in autoimmune disease and inflammation pathways, facilitating the study of RORγt as a therapeutic target. -
RORγ Inverse Agonist
RORγ inverse agonist 1 is an inverse agonist of the retinoic acid receptor-related orphan receptor gamma (RORγ). This compound modulates RORγ activity, negatively regulating its transcriptional activity. It is primarily utilized in research related to immune responses and inflammation, offering insights into potential therapeutic strategies targeting autoimmune diseases and related disorders.
