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.

Products
Background
Gene Data

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

Antagonists

Cat No Product Name / Activity
5656 DY 268
Potent FXR antagonist
5694 GSK 2033
Potent LXR antagonist
5854 SR 9238
Potent and selective LXR inverse agonist
6138 SR 9243
Selective LXR inverse agonist

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