LXR-like Receptors
Liver X receptors (LXRs) and farnesoid X receptors (FXRs) are members of the steroid analog-activated nuclear receptor subfamily, which form heterodimers with members of the retinoid X receptor family. There are two closely related isoforms of each of these enzymes; α and β.
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LXR-like Receptor Agonists |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 2563 | Fexaramine |
| Potent, selective farnesoid X receptor (FXR) agonist | |
| 2474 | GW 3965 hydrochloride |
| Orally active liver X receptor (LXR) agonist | |
| 2473 | GW 4064 |
| Selective farnesoid X receptor (FXR) agonist | |
| 3907 | 27-Hydroxycholesterol |
| LXR agonist; also ER partial agonist | |
| 2373 | T 0901317 |
| Potent liver X receptor (LXR) agonist; also CAR inverse agonist | |
| 5951 | WAY 252623 |
| Potent LXR agonist | |
LXR-like Receptor Inverse Agonists |
|
| Cat. No. | Product Name / Activity |
| 5854 | SR 9238 |
| Potent and selective LXR inverse agonist | |
| 6138 | SR 9243 |
| Selective LXR inverse agonist | |
LXR-like Receptor Antagonists |
|
| Cat. No. | Product Name / Activity |
| 5656 | DY 268 |
| Potent FXR antagonist | |
| 5694 | GSK 2033 |
| Potent LXR antagonist | |
Liver X receptors (LXRs) and farnesoid X receptors (FXRs) are members of the steroid analog-activated nuclear receptor subfamily, which form heterodimers with members of the retinoid X receptor family. There are two closely related isoforms of each of these enzymes; LXRα and LXRβ, and FXRα and FXRβ (pseudogene in man).
LXRα and FXRα expression is restricted to the liver, small intestine, kidney and adrenal gland, whilst LXRβ and FXRβ are ubiquitously expressed. Despite acting on some of the same target genes, including cholesterol 7α-hydroxylase (CYP7A1) and SREBP-1c, LXRs and FXRs have different physiological roles. LXRs are involved in cholesterol homeostasis, inhibition of proinflammatory gene expression in atherosclerosis and activation of innate immunity, whilst FXRs have a vital function in bile acid homeostasis.
External sources of pharmacological information for LXR-like Receptors :
LXR and FXR Gene Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|---|---|---|---|
| LXRα | Human | NR1H3 | NM_001130101 | Q13133 |
| Mouse | Nr1h3 | NM_013839 | Q9Z0Y9 | |
| Rat | Nr1h3 | NM_031627 | Q5I035 | |
| LXRβ | Human | NR1H2 | NM_007121 | P55055 |
| Mouse | Nr1h2 | NM_009473 | Q60644 | |
| Rat | Nr1h2 | NM_031626 | Q62755 | |
| FXRα | Human | NR1H4 | NM_005123 | Q96RI1 |
| Mouse | Nr1h4 | NM_009108 | Q60641 | |
| Rat | Nr1h4 | NM_021745 | Q5XI75 | |
| FXRβ | Human | NR1H5P | NG_007471.1 | - |
| Mouse | Nr1h5 | NM_198658 | NP_941060 |