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FXR+antagonist

" in MedChemExpress (MCE) Product Catalog:

23

Inhibitors & Agonists

10

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0172
    Lithocholic acid
    15+ Cited Publications

    3α-Hydroxy-5β-cholanic acid

    		 Autophagy Endogenous Metabolite Apoptosis FXR Metabolic Disease Inflammation/Immunology Cancer
    Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist .
    Lithocholic acid
  • HY-107738
    Guggulsterone
    Maximum Cited Publications
    21 Publications Verification

    Z/E-Guggulsterone

    		 Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively .
    Guggulsterone
  • HY-135103
    Tauro-β-muricholic acid sodium
    4 Publications Verification

    T-βMCA sodium

    		 FXR Cancer
    Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM .
    Tauro-β-muricholic acid sodium
  • HY-110066
    (Z)-Guggulsterone
    5+ Cited Publications

    		 Apoptosis VEGFR Akt Angiotensin-converting Enzyme (ACE) SARS-CoV FXR Cardiovascular Disease Cancer
    (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis . (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection .
    (Z)-Guggulsterone
  • HY-110267
    DY268
    3 Publications Verification

    		 FXR Metabolic Disease
    DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI) .
    DY268
  • HY-N9933
    Tauro-β-muricholic acid
    4 Publications Verification

    TβMCA

    		 FXR Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Tauro-β-muricholic acid (TβMCA) is an orally active trihydroxylated bile acid and a competitive, reversible FXR antagonist (IC50=40 μM). Tauro-β-muricholic acid inhibits bile acid-induced hepatocyte apoptosis by maintaining mitochondrial membrane potential, while simultaneously inhibiting intestinal FXR signaling, affecting bile acid synthesis, hepatic lipid metabolism, and insulin sensitivity. Accumulation of tauro-β-muricholic acid disrupts metabolic homeostasis, promoting cancer stem cell proliferation and tumor progression. The mechanisms of tauro-β-muricholic acid involve two aspects: first, inhibiting the translocation of the pro-apoptotic protein Bax to mitochondria and maintaining mitochondrial membrane potential (MMP); and second, blocking the FXR signaling pathway to regulate bile acid metabolism, reduce serum ceramide production, and downregulate the hepatic SREBP1C/CIDEA pathway. Tauro-β-muricholic acid possesses anti-hepatocyte apoptosis, bile acid homeostasis regulation, and liver fat accumulation reduction properties, and also functions as a biomarker, making it useful in the study of diseases such as bile acid metabolism disorders, non-alcoholic fatty liver disease, colorectal cancer, and liver fibrosis .
    Tauro-β-muricholic acid
  • HY-B0172R
    Lithocholic acid (Standard)
    15+ Cited Publications

    3α-Hydroxy-5β-cholanic acid (Standard)

    		 Reference Standards Autophagy Endogenous Metabolite Apoptosis FXR Metabolic Disease Cancer
    Lithocholic acid (Standard) is the analytical standard of Lithocholic acid. This product is intended for research and analytical applications. Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist .
    Lithocholic acid (Standard)
  • HY-133890
    Tauro-α-muricholic acid
    2 Publications Verification

    T-α-MCA

    		 Endogenous Metabolite FXR Neurological Disease Metabolic Disease
    Tauro-α-muricholic acid (T-α-MCA) is a Taurine (HY-B0351)-conjugated primary Bile acid. Tauro-α-muricholic acid is a FXR antagonist with an IC50 of  28 µM. Tauro-α-muricholic acid attenuates other bile acid-activated FXR signaling. Tauro-α-muricholic acid can be used in the research of Alzheimer's disease, glucose metabolism, and lipid metabolism .
    Tauro-α-muricholic acid
  • HY-151481
    FXR antagonist 1

    		FXR Metabolic Disease
    FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
    FXR antagonist 1
  • HY-N0910
    Notoginsenoside Ft1
    1 Publications Verification

    		 PI3K mTOR Akt Apoptosis p38 MAPK ERK Transmembrane Glycoprotein Glutathione Reductase (GR) Estrogen Receptor/ERR Calcium Channel Ferroptosis G protein-coupled Bile Acid Receptor 1 FXR Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Notoginsenoside Ft1 is an orally active bioactive saponin. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8 + T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca 2+ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y12 receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance .
    Notoginsenoside Ft1
  • HY-133890A
    Tauro-α-muricholic acid sodium
    2 Publications Verification

    T-α-MCA sodium

    		 Endogenous Metabolite FXR Neurological Disease Metabolic Disease
    Tauro-α-muricholic acid sodium (T-α-MCA sodium) is a Taurine (HY-B0351)-conjugated primary Bile acid. Tauro-α-muricholic acid sodium is a FXR antagonist with an IC50 of  28 µM. Tauro-α-muricholic acid sodium attenuates other bile acid-activated FXR signaling. Tauro-α-muricholic acid sodium can be used in the research of Alzheimer's disease, glucose metabolism, and lipid metabolism .
    Tauro-α-muricholic acid sodium
  • HY-148874A
    FXR antagonist 2 hydrochloride

    		FXR Metabolic Disease
    FXR antagonist 2 (compound A-26) hydrochloride is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 hydrochloride can be used in the study of hyperlipidemia and type 2 diabetes .
    FXR antagonist 2 hydrochloride
  • HY-163436
    F44-A13

    		FXR Cytochrome P450 RAR/RXR PPAR ROR Metabolic Disease
    F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders .
    F44-A13
  • HY-148874
    FXR antagonist 2

    		FXR Metabolic Disease
    FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes .
    FXR antagonist 2
  • HY-151481A
    β-FXR antagonist 1

    		FXR Neurological Disease
    β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist .
    β-FXR antagonist 1
  • HY-163072
    FXR antagonist 3

    		FXR Metabolic Disease
    FXR antagonist 3 (V02-8) is an intestine-specific farnesoid X receptor (FXR) antagonist, with an IC50 of 0.89 μM .
    FXR antagonist 3
  • HY-B1734
    16-Dehydropregnenolone acetate

    16-DPA

    		 FXR 5 alpha Reductase Cytochrome P450 Drug Intermediate Cardiovascular Disease Cancer
    16-Dehydropregnenolone acetate (16-DPA), a sterols compound, is an orally active 17α-hydroxylase and 5α-reductase inhibitor. 16-Dehydropregnenolone is also a potent bile acid receptor (BAR)/farnesoid X receptor (FXR) antagonist. 16-Dehydropregnenolone hypolipidemic and anticancer effects. 16-Dehydropregnenolone acetate (16-DPA) is the drug intermediate that can be used for synthesis of Dexamethasone (HY-14648) and related other steroidal pharmacophores .
    16-Dehydropregnenolone acetate
  • HY-110066R
    (Z)-Guggulsterone (Standard)

    		Reference Standards Apoptosis VEGFR Akt Angiotensin-converting Enzyme (ACE) SARS-CoV FXR Cancer
    (Z)-Guggulsterone (Standard) is the analytical standard of (Z)-Guggulsterone. This product is intended for research and analytical applications. (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis . (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection .
    (Z)-Guggulsterone (Standard)
  • HY-107738R
    Guggulsterone (Standard)

    Z/E-Guggulsterone (Standard)

    		 Apoptosis JNK Akt Caspase FXR Autophagy Reference Standards Cancer
    Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
    Guggulsterone (Standard)
  • HY-183279
    FXR antagonist 4

    		FXR AMPK Metabolic Disease
    FXR antagonist 4 (Compound 4l) is an orally active, selective FXR antagonist with an IC50 of 0.70 μM. FXR antagonist 4 binds to FXR, differentially regulates bile acid and lipid transporter genes, and exerts no effect on gluconeogenesis-related genes. FXR modulator 1 activates the AMPK signaling pathway to inhibit fatty acid synthesis. FXR modulator 1 alleviates hepatic steatosis, ballooning degeneration and fibrosis, and improves dyslipidemia. FXR modulator 1 can be used for research on metabolic dysfunction-associated steatohepatitis .
    FXR antagonist 4
  • HY-135103S
    Tauro-β-muricholic acid-d4 sodium

    		Isotope-Labeled Compounds FXR Cancer
    Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM .
    Tauro-β-muricholic acid-d4 sodium
  • HY-133890AS
    Tauro-α-muricholic acid-d4 sodium

    T-α-MCA-d4 sodium

    		 Isotope-Labeled Compounds Endogenous Metabolite FXR Neurological Disease Metabolic Disease
    Tauro-α-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-α-muricholic acid sodium (HY-133890A). Tauro-α-muricholic acid sodium (T-α-MCA sodium) is a Taurine (HY-B0351)-conjugated primary Bile acid. Tauro-α-muricholic acid sodium is a FXR antagonist with an IC50 of  28 µM. Tauro-α-muricholic acid sodium attenuates other bile acid-activated FXR signaling. Tauro-α-muricholic acid sodium can be used in the research of Alzheimer's disease, glucose metabolism, and lipid metabolism .
    Tauro-α-muricholic acid-d4 sodium
  • HY-181876
    F44-S101

    		FXR Metabolic Disease
    F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia .
    F44-S101

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