orphan receptor

RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

LRH-1 Inhibitor-3 is an antagonist that inhibits LRH-1 transcriptional activity, reducing the expression of target genes associated with cell growth and proliferation, such as SHP (small heterodimer partner), cyclin E1 (CCNE1), and G0S2, and inhibiting the proliferation of human pancreatic, colon, and breast adenocarcinoma cells.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

NR2F6 modulator-2 (Compound I) is an effective NR2F6 modulator that inhibits the recruitment of endogenous NSD1 peptides, with an IC50 equivalent to 2 equivalents of NR2F6. It is applicable in cancer and immunology research.

DLPC is an LRH-1 agonist ligand. DLPC is a phospholipid for biological study[1][2].

NR2E3 agonist 1 is a small molecule photoreceptor-specific nuclear receptor (NR2E3) agonist with antitumor activity for the study of diseases caused by abnormalities in photoreceptor cell-specific receptors.

ML179 is a potent and selective inverse agonist of liver receptor homolog-1 (LRH1, NR5A2) with IC50 of 320 nM.

(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.

AF64394 is a selective inverse agonist of GPR3(pIC50 : 7.3)

CID 1375606 is a surrogate agonist of the orphan G protein-coupled receptor [GPR27], characterized by a high level of conservation among vertebrates and predominant expression in the central nervous system.

'(Des-Bromo)-Neuropeptide B (1-23) (human)' is an agonist for orphan G-protein-coupled receptors, exhibiting a K i of 1.2 nM for GPR7 (NPBW1) and 341 nM for GPR8 (NPBW2) respectively [1].

7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is an LRH-1 antagonist with an IC50 of 3.1 μM.

N-(3-Chloro-4-morpholinophenyl)-N'-hydroxyformimidamide (TS-011) is a selective 20-Hydroxyeicosatetraenoic acid synthesis inhibitor.

TLX agonist 2 (compound 31) is a TLX agonist with an EC50 of 0.1 μM and a Kd of 0.16 μM. This compound enhances transcriptional activity by binding to TLX, thereby boosting the expression of TLX target genes. TLX agonist 2 is utilized in research on neurodegenerative diseases.

GPR27 agonist-1 (compound I) is a selective agonist for GPR27 with a pEC50 value of 6.34.

Anticanceragent 258 is an imidazo[1,2-B][1,2,4]triazole derivative that modulates nuclear receptor activity. It exhibits an EC50 of 63 nM for Nurr in N2A cells and an IC50 of 0.1 pM for Nur77 in HEK293 cells. Anticanceragent 258 is applicable in studies related to cancer, metabolic disorders, and neurological diseases.

PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.

LysoPalloT-NH-amide-C3-ph-m-O-C11 is an agonist of the GPR174 receptor with an EC50 value of 34 nM.

SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.

20-SOLA is the first water-soluble 20-HETE antagonist with oral bioavailability. It significantly improves blood pressure changes and kidney damage associated with the streptozotocin (STZ) diabetic mouse model. Additionally, 20-SOLA acts as a GPR75 receptor blocker. This compound is useful in research related to cardiovascular pathology.

BI 6015 is an antagonist of HNF4α. HNF4α is a nuclear receptor that regulates gene expression in the intestine cells, liver cells, and pancreas-β cells.

SID 7969543 is a selective SF-1 inhibitor with potential anticancer activity, inhibits SF-1-triggered luciferase expression and can be used for cancer research.

BMH-9 is an RNA polymerase I inhibitor that acts by causing nucleolar stress and showing potent anticancer activity across many tumor types.

Photoregulin1 is a modulator of Nr2e3. Photoregulin1 slows the progression of photoreceptor degeneration in two common mouse models of autosomal dominant RP, the RhoP23H and the Pde6brd1 mutations.