ROR

Cat. No.

A40182

CAS No.

1414248-06-8

SR-1903

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.

Cat. No.

A41739

CAS No.

2460400-11-5

Ozuriftamab vedotin

Synonyms: BA3021; Anti-ROR2 ADC; CAB-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.

Cat. No.

A41753

CAS No.

2765612-38-0

BL20-MMAE

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.

Cat. No.

A50662

CAS No.

2299252-72-3

Izumerogant

Synonyms: IMU-935

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.

Cat. No.

A53528

CAS No.

3000567-45-0

RORγ/DHODH-IN-2

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.

Cat. No.

A60389

CAS No.

2276-94-0

Allolithocholic acid

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.

Cat. No.

A61728

CAS No.

87958-67-6

CGP52608

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.

Cat. No.

A70040

CAS No.

2764662-15-7

RORγt/DHODH-IN-1

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.

Cat. No.

A70041

CAS No.

2764662-16-8

RORγt/DHODH-IN-3

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.

Cat. No.

A70044

CAS No.

2641758-86-1

RORγt/DHODH-IN-2

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.

Cat. No.

A71597

CAS No.

566-97-2

Zymostenol

Synonyms: 5a-Cholest-8-en-3b-ol

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.

Cat. No.

A77553

CAS No.

1553-56-6

3-Oxo-5β-cholanoic acid

Synonyms: Dehydrolithocholic acid; 3-oxoLCA

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.

Cat. No.

A77554

CAS No.

1426802-50-7

GSK805

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.

Cat. No.

A77555

CAS No.

17676-33-4

Neoruscogenin

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.

Cat. No.

A77556

CAS No.

1873358-87-2

XY018

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.

Cat. No.

A77557

CAS No.

1817773-66-2

Bevurogant

Synonyms: BI 730357

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.

Cat. No.

A77559

CAS No.

1392809-08-3

MRL-871

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.

Cat. No.

A77560

CAS No.

1917306-14-9

JNJ-61803534

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.

Cat. No.

A77561

CAS No.

529500-72-9

RORγ inverse agonist 1

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.

Cat. No.

A77562

CAS No.

3053223-31-4

LDR102

LDR102 is a potent inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) with a Ki value of 0.10 μM. This compound effectively inhibits the proliferation of various cancer cell lines, including H1975, A549, and MDA-MB-231, exhibiting IC50 values of 0.36 μM, 1.37 μM, and 0.47 μM, respectively. Additionally, LDR102 demonstrates antitumor efficacy in murine models and displays favorable pharmacokinetic properties in rat studies, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A77563

CAS No.

2170477-75-3

RORγt inverse agonist 13

RORγt inverse agonist 13 is a selective inverse agonist targeting the RORγt receptor with an IC50 of 63.8 nM. This compound demonstrates potent biological activity, making it suitable for research applications focusing on autoimmune diseases and T cell differentiation. Its improved agent-like properties enhance its utility in preclinical studies investigating the modulation of RORγt signaling pathways.

Cat. No.

A77564

CAS No.

1386439-51-5

SR1555

SR1555 is a specific inverse agonist of the retinoic acid receptor-related orphan nuclear receptor γ (RORγ), exhibiting an IC50 value of 1 μM. This compound is known to effectively inhibit TH17 cell development and function while promoting an increase in T regulatory cell frequency and downregulating IL-17 expression. SR1555 is valuable for investigating mechanisms in autoimmune disease research.

Cat. No.

A77565

CAS No.

1334526-14-5

(±)-ML 209

(±)-ML 209 is a selective RORγ antagonist that effectively inhibits RORγt transcriptional activity, demonstrating an IC50 of 300 nM in HEK293t cells. This diphenylpropanamide compound specifically suppresses murine Th17 cell differentiation while leaving the differentiation of naïve CD4+ T cells into Th1 and regulatory T cell lineages unaffected. Its unique mechanism makes (±)-ML 209 a valuable tool for researchers investigating the role of RORγ in immune responses and related diseases.

Cat. No.

A77566

CAS No.

240129-43-5

7ß,27-Dihydroxycholesterol

Synonyms: 7β; 27-OHC

7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a selective activator of RORγt, exhibiting a Ki of 120 nM. This compound plays a crucial role in promoting the differentiation of CD4+ Th17 cells in both mouse and human models. Additionally, 7ß,27-Dihydroxycholesterol enhances IL-17 production through a CYP27A1-dependent pathway, making it valuable for studies focused on immune response and related signaling pathways.

Cat. No.

A77567

CAS No.

2055496-11-0

Cedirogant

Synonyms: ABBV-157

Cedirogant is an orally active inverse agonist of the retinoic acid receptor-related orphan receptor gamma-t (RORγt). It demonstrates significant potential in modulating immune responses, particularly in the context of psoriasis research. This compound serves as a valuable tool for investigating therapeutic strategies targeting autoimmune and inflammatory conditions.