LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes[1].
Nagilactone B, extracted from the root bark of Podocarpus nagi, is a liver X receptor (LXR) agonist.
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
AZ876 is a novel high-affinity LXR agonist. AZ876 was 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.(1) AZ876 suppressed up-regulation of hypertrophy- and fibrosis-related genes, and further inhibited prohypertrophic and profibrotic transforming growth factor β (TGFβ)-Smad2/3 signalling.(2) AZ876 prevented TGFβ- and angiotensin II-induced fibroblast collagen synthesis, and inhibited up-regulation of the myofibroblastic marker, α-smooth muscle actin.(3) The reference for administration is 20 umol/kg/day in vivo.
GAC0003A4 is a novel LXR inverse agonist, functioning as LXR a degrader"
RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
Iristectorigenin B (Iristectrigenin B) is a liver X receptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β[1].
22(R)-Hydroxycholesterol (Narthesterol) is an endogenous LXR agonist. 22(R)-Hydroxycholesterol (Narthesterol) can be used for tangier disease research[1].
RGX-104 (free base) is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
GAC0001E5 is a novel LXR inverse agonist, functioning as LXR a degrader"
Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels[1].
24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation[1].
GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
GW6340 is an intestinal-specific LXR agonist. GW6340 promotes macrophage reverse cholesterol transport (mRCT)[1].
BMS-852927 is an LXRβ-selective agonist.
LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma[1].
GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
Saikosaponin A is an active component of Bupleurum falcatum, up-regulates LXRα expression, with potent anti-inflammatory activity[1].
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators[1][2][3].
T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively.
27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis[1].
Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br[1]. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression[2].
SR9238 is a synthetic LXR antagonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis[1].
FITC-GW3965 is a fluorescence-labelled liver X receptor β (LXRβ) agonist GW3965 (HY-10627). FITC-GW3965 is a tracer, that can be designed by replacing the trifluoromethyl of GW3965 with an amide to link the FITC. FITC-GW3965 can be used to study the function of LXRβ[1].