LXR Antagonist

GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively.

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC₅₀s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC₅₀ of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer.

GAC0001E5 is an LXR inverse agonist. GAC0001E5 has antiproliferative activity and can be used in cancer research.

Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models.

BE1218 is a liver X receptor (LXR) inverse agonist with IC₅₀ values of 9 nM and 7 nM against LXRα and LXRβ, respectively.

Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. 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.

Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC₅₀ of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models.

TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver.

Larsucosterol (DUR-928) ammonium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol ammonium as a potent endogenous regulator decreases lipogenesis. Larsucosterol ammonium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.

SR9238 (Standard) is the analytical standard of SR9238. This product is intended for research and analytical applications. SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

Yamogenin (Standard) is the analytical standard of Yamogenin. This product is intended for research and analytical applications. Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC₅₀ of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer.

GSK2033 (Standard) is the analytical standard of GSK2033 (HY-108688). This product is intended for research and analytical applications. GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively.