NR1
Non-steroid nuclear receptors include thyroid hormone receptor, retinoic acid receptor, vitamin D receptor, Liver X receptor like receptors (LXR and FXR) and PPARγ. Members of this family heterodimerize with the retinoid X receptor (RXR). Prior to ligand binding, receptor heterodimers are located in the nucleus as part of complexes with histone deacetylases (HDACs) and other corepressors that keep target DNA in a tightly wound conformation, preventing exposure to transactivation factors. Ligand binding results in HDAC dissociation, chromatin derepression, and transcriptional activation.In addition to ligand binding, nuclear receptor activity can be modulated through the action of numerous growth factor and cytokine signaling cascades that result in receptor phosphorylation or other post-translational modifications, typically within the N-terminal transactivation domain. [1].
[1] P. Germain et al. Overview of nomenclature of nuclear receptors. Pharmacol. Rev. 2006, 58, 685-704.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2948 | AM 580 | RAR-α agonist | €95.00 | |
| 2679 | AR7 | RARα antagonist that stimulates chaperone-mediated autophagy | €90.00 | |
| 3904 | BAY-0069 | Potent covalent PPARγ inverse agonist | €90.00 | |
| 3809 | BAY-4931 | Potent covalent PPARγ inverse agonist | €120.00 | |
| 1194 | BMS 189961 | RAR-γ agonist | €145.00 | |
| 1173 | BMS 270394 | RAR-γ agonist | €165.00 | |
| 1676 | BXL 628 | Vitamin D receptor (VDR) agonist | €150.00 | |
| 2964 | CD12681 | Potent RORγ inverse agonist | €135.00 | |
| 1950 | CDDO | A potent multifunctional anti-tumor agent. PPAR-γ agonist | €80.00 | |
| 1241 | CH 55 | RAR agonist | €90.00 | |
| 2114 | CP 775146 | Potent and selective PPARα agonist | €85.00 | |
| 3021 | DL5050 | Potent and highly selective hCAR agonist | €140.00 | |
| 1746 | Doxercalciferol | Vitamin D2 analog, VDR agonist | €100.00 | |
| 2561 | DY 268 | Highly potent FXR antagonist with a promising in vitro profile | €120.00 | |
| 2727 | Elafibranor | Dual PPARα/δ agonist | €90.00 | |
| 2686 | FH535 | Dual inhibitor of PPAR and Wnt/β-catenin signaling | €75.00 | |
| 2706 | FH535 sodium salt | Dual inhibitor of PPAR and Wnt/β-catenin signaling | €80.00 | |
| 2363 | GSK 2033 | The first potent cell-active LXR antagonist | €105.00 | |
| 1628 | GSK 3787 | PPARδ antagonist | €90.00 | |
| 1266 | GW 3965 hydrochloride | Liver X receptor agonist | €95.00 | |
| 1237 | GW 7647 | PPARα agonist | €95.00 | |
| 2262 | GW 9662 | Selective PPARγ antagonist | €60.00 | |
| 2533 | Hydroxypioglitazone | Active metabolite of Pioglitazone (M-IV), a PPARγ agonist | €180.00 | |
| 2019 | INT131 | Selective PPARγ modulator (partial agonist) | €90.00 | |
| 1567 | KRP 297 | PPARα agonist; PPARγ agonist | €110.00 | |
| 1242 | LE 135 | RAR antagonist | €120.00 | |
| 2357 | LXR 623 | Partial agonist of Liver X Receptor | €95.00 | |
| 2637 | LY 2955303 dihydrochloride | Potent and selective RARγ antagonist for the treatment of osteoarthritis pain | €145.00 | |
| 3740 | LYC-55716 | Potent RORγ agonist | Inquire | |
| 2657 | MGL-3196 | Oral, liver-targeted, selective thyroid hormone receptor β-agonist | €90.00 | |