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RORγt inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Dihydroorotate Dehydrogenase (3) Fluorescent Dye (1) GPR39 (1) Interleukin Related (3) Isotope-Labeled Compounds (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) ROR (26) STAT (1)
By Research Areas:	Cancer (1) Inflammation/Immunology (27) Metabolic Disease (1) Neurological Disease (1)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-125801

3-Oxo-5β-cholanoic acid 1 Publications Verification Dehydrolithocholic acid; 3-oxoLCA	ROR	Inflammation/Immunology
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (K_d=1.13 μM) .

HY-12776

GSK805 5 Publications Verification	ROR	Inflammation/Immunology
GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC₅₀ values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .

HY-113238A

Lithocholic acid 3-sulfate disodium Sulfolithocholic acid disodium; LCAS disodium	GPR39 ROR	Metabolic Disease Inflammation/Immunology
Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

HY-139780

JNJ-61803534	ROR	Inflammation/Immunology
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 .

HY-126037

(±)-ML 209 1 Publications Verification	ROR	Inflammation/Immunology
(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC₅₀ of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC₅₀ of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 ⁺ T cells into other lineages, including Th1 and regulatory T cells .

HY-117819

TMP920	ROR	Inflammation/Immunology
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC₅₀ of 0.03 μM .

HY-119366

S18-000003	ROR	Inflammation/Immunology
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 .

HY-142834

RORγt/DHODH-IN-2	ROR Dihydroorotate Dehydrogenase	Inflammation/Immunology
RORγt/DHODH-IN-2 (compound 1) is a potent dual *RORγt/DHODH* inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research .

HY-103637

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

HY-142934

*RORγt inhibitor* 2**	ROR	Inflammation/Immunology Cancer
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC₅₀ of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt .

HY-136527

BMS-986251	ROR Interleukin Related	Inflammation/Immunology
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC₅₀ of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC₅₀ of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .

HY-103637A

Vimirogant hydrochloride 1 Publications Verification VTP-43742 hydrochloride	ROR	Inflammation/Immunology
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 .

HY-162490

TF-S14	ROR	Inflammation/Immunology
TF-S14 is a reverse agonist of RORγt. TF-S14 reduces Th17 cell-associated cytokine production, including IL-17A, IL-21, and IL-22 by binding to and inhibiting RORγt activity. TF-S14 can be used in the study of autoimmune diseases and rejection in allotransplantation .

HY-19510

*RORγt inhibitor* 4**	ROR	Neurological Disease Inflammation/Immunology
RORγt inhibitor 4 (Compound 9a) is an orally active and a CNS-penetrating RORγt inhibitor. RORγt inhibitor 4 improves experimental autoimmune encephalomyelitis .

HY-142296

*RORγt inhibitor* 1**	ROR	Inflammation/Immunology
RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC₅₀ value of 1 nM.

HY-112863

*RORγt inhibitor* 3**	ROR	Inflammation/Immunology
RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitory activity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .

HY-142703

RORγt inverse agonist 28	ROR	Inflammation/Immunology
RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .

HY-142806

RORγt inverse agonist 26	ROR	Inflammation/Immunology
RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .

HY-142938

RORγt agonist 3	ROR	Inflammation/Immunology
RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23) .

HY-142937

RORγt agonist 2	ROR	Inflammation/Immunology
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17) .

HY-142847

RORγt/DHODH-IN-3	ROR Dihydroorotate Dehydrogenase	Inflammation/Immunology
RORγt/DHODH-IN-3 (compound (S)-14d) is a dual *RORγt/DHODH* inhibitor, with IC₅₀s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity .

HY-176273

RORγt inverse agonist 35	ROR Interleukin Related	Inflammation/Immunology
RORγt inverse agonist 35 (Compound 22) is a RORγt inverse agonist with an IC₅₀ of 1.51 μM. RORγt inverse agonist 35 significantly inhibits Th17 differentiation and proinflammatory properties in human CD4 ⁺ T cells. RORγt inverse agonist 35 can be used for research of Th17-driven autoimmune diseases, such as psoriasis, multiple sclerosis, and inflammatory bowel disease (IBD) .

HY-142843

RORγt/DHODH-IN-1	ROR Dihydroorotate Dehydrogenase	Inflammation/Immunology
RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual *RORγt/DHODH* inhibitor, with IC₅₀s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity .

HY-113238F

FITC-Lithocholic acid 3-sulfate FITC-Sulfolithocholic acid	Fluorescent Dye	Others
FITC-Lithocholic acid 3-sulfate (FITC-Sulfolithocholic acid) is a FITC-labeled Lithocholic acid 3-sulfate, which is a sulfated biliary metabolite. Lithocholic acid 3-sulfate selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate can be used for the research of pathogenesis of cholestatic liver diseases .

HY-125801R

3-Oxo-5β-cholanoic acid (Standard) Dehydrolithocholic acid (Standard); 3-oxoLCA (Standard)	Reference Standards ROR	Inflammation/Immunology
3-Oxo-5β-cholanoic acid (Standard) is the analytical standard of 3-Oxo-5β-cholanoic acid. This product is intended for research and analytical applications. 3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM)[1].

HY-N16465

Cinnamtannin D1	Apoptosis Reactive Oxygen Species (ROS) STAT	Inflammation/Immunology
Cinnamtannin D1 is an orally active polyphenolic compound with immunosuppressive activity. Cinnamtannin D1 regulates the balance of Th17/Treg cells by inhibiting AHR expression. Cinnamtannin D1 reduces apoptosis and ROS in INS-1 cells and primary cultured murine islets induced by Palmitic acid (PA) (HY-N0830). Cinnamtannin D1 reduces Th17 cell differentiation via downregulating *p-STAT3*/RORγt and promotes Treg cell differentiation via upregulating p-STAT5/Foxp3. Cinnamtannin D1 exerts excellent anti-arthritic efficacy in collagen-induced arthritis (CIA) model of mice. Cinnamtannin D1 can be used for the study of rheumatoid arthritis (RA) .

HY-183763

RORγt inverse agonist 37	ROR Interleukin Related	Inflammation/Immunology
RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC₅₀ of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation .

HY-125801S

3-Oxo-5β-cholanoic acid-d4 Dehydrolithocholic acid-d₄; 3-oxoLCA-d₄	Isotope-Labeled Compounds ROR	Inflammation/Immunology
3-Oxo-5β-cholanoic acid-d₄ (Dehydrolithocholic acid-d₄) is the deuterium labeled 3-Oxo-5β-cholanoic acid (HY-125801). 3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (K_d=1.13 μM) .

FITC-Lithocholic acid 3-sulfate FITC-Sulfolithocholic acid	Fluorescent Dyes
FITC-Lithocholic acid 3-sulfate (FITC-Sulfolithocholic acid) is a FITC-labeled Lithocholic acid 3-sulfate, which is a sulfated biliary metabolite. Lithocholic acid 3-sulfate selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate can be used for the research of pathogenesis of cholestatic liver diseases .

Cat. No.	Product Name	Type

HY-113238A

Lithocholic acid 3-sulfate disodium Sulfolithocholic acid disodium; LCAS disodium	Biochemical Assay Reagents
Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

Lithocholic acid 3-sulfate disodium

Sulfolithocholic acid disodium; LCAS disodium

Biochemical Assay Reagents

Lithocholic acid 3-sulfate disodium is a GPR39 agonist, with EC₅₀ values of 41 μM and 42.4 μM in M39-20 and hGPR39-2 cells, respectively, in the absence of Zn ²⁺, and 0.88 μM and 0.97 μM in the presence of Zn ²⁺. Lithocholic acid 3-sulfate disodium acts as a RORγt ligand. Lithocholic acid 3-sulfate disodium stimulates the GPR39 receptor to initiate intracellular calcium signaling, independent of the Zn ²⁺-binding sites H17 and H19. LCA-3-S selectively inhibits Th17 cell differentiation by targeting RORγt. Lithocholic acid 3-sulfate disodium can be used in the research of cholestatic liver diseases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N16465

Cinnamtannin D1	Phenols Polyphenols Plants Lauraceae Lindera glauca (Siebold & Zucc.) Blume Source Classification	Apoptosis Reactive Oxygen Species (ROS) STAT
Cinnamtannin D1 is an orally active polyphenolic compound with immunosuppressive activity. Cinnamtannin D1 regulates the balance of Th17/Treg cells by inhibiting AHR expression. Cinnamtannin D1 reduces apoptosis and ROS in INS-1 cells and primary cultured murine islets induced by Palmitic acid (PA) (HY-N0830). Cinnamtannin D1 reduces Th17 cell differentiation via downregulating *p-STAT3*/RORγt and promotes Treg cell differentiation via upregulating p-STAT5/Foxp3. Cinnamtannin D1 exerts excellent anti-arthritic efficacy in collagen-induced arthritis (CIA) model of mice. Cinnamtannin D1 can be used for the study of rheumatoid arthritis (RA) .

Cat. No.	Product Name	Chemical Structure

HY-125801S

3-Oxo-5β-cholanoic acid-d4
3-Oxo-5β-cholanoic acid-d₄ (Dehydrolithocholic acid-d₄) is the deuterium labeled 3-Oxo-5β-cholanoic acid (HY-125801). 3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (K_d=1.13 μM) .

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RORγt inhibitor

Inhibitors & Agonists

Fluorescent Dyes

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Isotope-Labeled Compounds

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