- Cat. No.
- A13193
SR1001
SR1001 is a selective ROR-alpha and ROR-gamma inverse agonist; suppresses TH17 cell differentiation and inhibits autoimmunity.
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ROR modulators target retinoic acid receptor-related orphan receptors (RORs), a family of nuclear receptors. The family has three members, RORα, RORβ and RORγ, which bind ROR response elements in target genes and are active without an added ligand. RORα contributes to circadian clock regulation, and the immune isoform RORγt directs the differentiation of interleukin-17 (IL-17)-producing T helper (Th17) cells. In 2011 the synthetic RORα/γ ligand SR1001 was shown to suppress Th17 differentiation and autoimmunity in mice. SR-2211 and XY101 act on RORγ, whereas SR3335 is selective for RORα. SR1078 is used as an agonist of RORα and RORγ in studies of target gene expression. Related receptors without well-defined ligands are listed under Orphan Nuclear Receptor.
SR1001 is a selective ROR-alpha and ROR-gamma inverse agonist; suppresses TH17 cell differentiation and inhibits autoimmunity.
SR-2211 selectively binds RORr(Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORr activity (IC50 = 320 nM).
SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ; increases transcription of RORα target genes; thought to increase p53 stability.
Synonyms: ML-176
SR3335 is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
RORγ modulator 1 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124.
Synonyms: LYC55716
LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist.
Synonyms: VTP-43742
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-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
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.
Synonyms: AZD0284.
AZD-0284 is a potent, selective, inverse agonist of the nuclear receptor RORγ for the potential treatment of Plaque psoriasis.
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release.
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.
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.
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM).
Synonyms: TMP 778??TMP-778
(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 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM.
Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.
GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC50 value of 13 nM for HEK-293 cell.
GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
Synonyms: TMP 778.
TMP778 is a novel, potent, and selective RORγt inverse agonist.
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.
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-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.
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