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FXR agonist

" in MedChemExpress (MCE) Product Catalog:

84

Inhibitors & Agonists

1

Peptides

12

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8

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0172
    Lithocholic acid
    Maximum Cited Publications
    20 Publications Verification

    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-50108
    GW 4064
    55+ Cited Publications

    FXR Autophagy Metabolic Disease Cancer
    GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
    GW 4064
  • HY-12222
    Obeticholic acid
    Maximum Cited Publications
    85 Publications Verification

    INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid

    FXR Autophagy Others
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
    Obeticholic acid
  • HY-10626
    T0901317
    40+ Cited Publications

    LXR FXR ROR Apoptosis Cardiovascular Disease Metabolic Disease Cancer
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
    T0901317
  • HY-10912
    Fexaramine
    5+ Cited Publications

    FXR Autophagy Others
    Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .
    Fexaramine
  • HY-109083
    Cilofexor
    5+ Cited Publications

    GS-9674

    FXR Autophagy Inflammation/Immunology
    Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research .
    Cilofexor
  • HY-107418
    Tropifexor
    5+ Cited Publications

    LJN452

    FXR Autophagy Cardiovascular Disease
    Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM .
    Tropifexor
  • HY-N4067

    isoCDCA

    FXR Endogenous Metabolite Metabolic Disease
    Isochenodeoxycholic acid (isoCDCA) is a FXR agonist. Isochenodeoxycholic acid activates the activity of FXR and induces the mRNA expression of FXR target genes (Ostβ and Kng1). Isochenodeoxycholic acid serves as a substrate for the liver class I ADH γγ isozyme-mediated 3β-dehydrogenation reaction .
    Isochenodeoxycholic acid
  • HY-50911
    Turofexorate isopropyl
    3 Publications Verification

    FXR-450; XL335; WAY-362450

    FXR Autophagy Metabolic Disease Cancer
    Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM .
    Turofexorate isopropyl
  • HY-109197
    Vonafexor
    2 Publications Verification

    EYP001

    FXR HBV Infection
    Vonafexor (EYP001) is an orally active, non-steroidal and selective FXR agonist. Vonafexor shows significant HBsAg reduction when combined with Peg-IFNα. Vonafexor can be used for anti-HBV research .
    Vonafexor
  • HY-160929

    CS-0159

    FXR Inflammation/Immunology
    Linafexor (CS-0159) is a FXR agonist and bile acid homeostasis modulator. Linafexor exerts its effects by activating FXR, a regulator of liver function. Linafexor is applicable to research related to primary sclerosing cholangitis (PSC). Linafexor is also suitable for research in the field of metabolic dysfunction-associated steatohepatitis (MASH) .
    Linafexor
  • HY-B0172R
    Lithocholic acid (Standard)
    Maximum Cited Publications
    20 Publications Verification

    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-151932
    FXR agonist 3
    1 Publications Verification

    FXR Inflammation/Immunology
    FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level .
    FXR agonist 3
  • HY-12434
    INT-767
    5+ Cited Publications

    FXR G protein-coupled Bile Acid Receptor 1 Autophagy Cancer
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively .
    INT-767
  • HY-N3431

    AMPK PD-1/PD-L1 FXR Reactive Oxygen Species (ROS) Cardiovascular Disease
    Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure .
    Kaempferol-7-O-rhamnoside
  • HY-109096

    LMB763

    FXR Autophagy Inflammation/Immunology
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH) .
    Nidufexor
  • HY-101273

    G protein-coupled Bile Acid Receptor 1 FXR Autophagy Neurological Disease Inflammation/Immunology
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-134988

    FXR Phosphatase Cytochrome P450 Inflammation/Immunology
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
    EDP-305
  • HY-147296

    MET409

    FXR Inflammation/Immunology Cancer
    Omesdafexor (MET409) is an orally active FXR agonist with a unique non-bile acid structure. Omesdafexor can be used for the study of non-alcoholic steatohepatitis (NASH) .
    Omesdafexor
  • HY-N4294

    FXR Insecticide Infection Metabolic Disease Inflammation/Immunology
    Arjungenin, a pentacyclic triterpenoid compound, is a FXR agonist. Arjungenin can improve insulin sensitivity by regulating the function of fat cells. Arjungenin exhibits moderate free radical scavenging activity. Arjungenin has growth inhibitory activity against the insect Spilarctia obliqua. Arjungenin has significant antiviral activity against a series of viruses such as chikungunya Virus (CHIKV) .
    Arjungenin
  • 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-151959

    FXR Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD) .
    FXR agonist 4
  • HY-142159

    FXR G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.
    FXR/TGR5 agonist 1
  • HY-169792

    FXR Aminotransferases (Transaminases) Metabolic Disease Inflammation/Immunology
    HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH) .
    HPG1860
  • HY-164799

    FXR Inflammation/Immunology
    FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models .
    FXR agonist 12
  • HY-135399

    FXR Inflammation/Immunology
    Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
    Tauro-obeticholic acid
  • HY-N3209

    FXR Inflammation/Immunology
    Nelumol A is a farnesoid X receptor (FXR) agonist .
    Nelumol A
  • HY-100443A
    trans-PX20606
    3 Publications Verification

    trans-PX-102

    FXR Autophagy Metabolic Disease
    PX20606 trans racemate (PX-102 trans racemate) is a FXR agonist with EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively .
    trans-PX20606
  • HY-103704

    FXR Autophagy Metabolic Disease
    LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM .
    LY2562175
  • HY-N3891

    FXR Inflammation/Immunology
    Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity .
    Fargesone A
  • HY-12222R

    INT-747 (Standard); 6-ECDCA (Standard); 6-Ethylchenodeoxycholic acid (Standard)

    Reference Standards FXR Autophagy Others
    Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
    Obeticholic acid (Standard)
  • HY-139418

    FXR Cancer
    PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models .
    PX20350
  • HY-153525

    FXR Metabolic Disease Inflammation/Immunology
    FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation .
    FXR agonist 5
  • HY-163466

    FXR Inflammation/Immunology
    FXR agonist 7 (compound 33) is a potent agonist of FXR, with EC50 of 0.1 nM. FXR agonist 7 shows high intestinal distribution, good anti-inflammatory activity .
    FXR agonist 7
  • HY-178959

    FXR Metabolic Disease Inflammation/Immunology
    FXR agonist 13 is a selective, orally active, potent FXR agonist (EC50 = 0.097 μM) and has favorable hepatic microsomal metabolic stability. FXR agonist 13 exhibits moderate affinity for FXR-LBD upon direct binding (KD = 14.74 μM). FXR agonist 13 displays good selectivity against related nuclear receptors, including LXRα/β, PPARα/γ/δ, PXR, and TGR5. FXR agonist 13 can be used for the study of metabolic-associated steatohepatitis (MASH) .
    FXR agonist 13
  • HY-168332

    FXR Metabolic Disease
    FXR agonist 11 (Compound 14) is an FXR agonist with an EC50 of 1.2 μM and a maximum effect of 73.7%. FXR agonist 11 can significantly increase GSH levels in the liver and is used to study drug-induced liver injury diseases .
    FXR agonist 11
  • HY-175516

    FXR PPAR Inflammation/Immunology
    dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model .
    dual FXR/PPARδ agonist-2
  • HY-168629

    FXR Metabolic Disease
    FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD and CCl4(HY-Y0298)-induced metabolic dysfunction-associated steatohepatitis mice .
    FXR agonist 9
  • HY-W587537

    FXR Metabolic Disease
    Deoxycholic Acid 3-O-beta-D-Glucuronide disodium salt is a bile acid receptor (FXR) agonist.
    Deoxycholic acid 3-O-β-D-glucuronide disodium
  • HY-100443

    PX-102

    FXR Cancer
    PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy .
    PX20606
  • HY-N10640

    FXR Inflammation/Immunology
    Alismanol M is a farnesoid X receptor (FXR) agonist with an EC50 value of 50.25 μM. Alismanol M is a protostane-type triterpenoid that can be isolated from the rhizome of Alisma orientale. Alismanol M can be used for the research of cholestasis and nonalcoholic steatohepatitis .
    Alismanol M
  • HY-W587451

    OCA-3-glucuronide disodium

    FXR Metabolic Disease
    Cholic acid 3-O-glucuronide (OCA-3-glucuronide) disodium is a farnesoid X receptor (FXR) agonist with an EC50 value of 91.5 μM. Cholic acid 3-O-glucuronide is promising for research of bile acid metabolism and detoxification .
    Cholic acid 3-O-glucuronide disodium
  • HY-12222S

    INT-747-d5; 6-ECDCA-d5; 6-Ethylchenodeoxycholic acid-d5

    FXR Autophagy Others
    Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
    Obeticholic acid-d5
  • HY-113567

    FXR Metabolic Disease
    GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively .
    GSK2324
  • HY-179278

    LXR Cardiovascular Disease Metabolic Disease Endocrinology
    LXR agonist 4 is a selective LXR inverse agonist with IC50 values of 7.6 (LXRα) and 2.9 μM (LXRβ), respectively. LXR agonist 4 exhibits selectivity over RORα and FXR. LXR agonist 4 robustly suppresses SREBP1c expression without altering ABCA1 or APOE. LXR agonist 4 displays antilipogenic properties and resolves fatty acid-induced steatosis. LXR agonist 4 can be used for the research of atherosclerosis and metabolic dysfunction-associated steatotic liver disease (MASLD) .
    LXR agonist 4
  • HY-10626R

    Reference Standards LXR FXR ROR Apoptosis Cardiovascular Disease Metabolic Disease Cancer
    T0901317 (Standard) is the analytical standard of T0901317. This product is intended for research and analytical applications. T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
    T0901317 (Standard)
  • HY-153114

    FXR Inflammation/Immunology
    HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
    HEC96719
  • HY-125996

    FXR Inflammation/Immunology
    NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease .
    NR1H4 activator 1
  • HY-181761

    FXR Metabolic Disease
    FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury .
    FXR agonist 16
  • HY-180221

    FXR Metabolic Disease
    FXR agonist 14 (Compound V15) is a partial, selective, orally active FXR agonist with an EC50 of 0.67 nM. FXR agonist 14 ameliorates pathological features in high-fat and high-sugar diet-induced MASH mice. FXR agonist 14 shows significant anti-cholestatic liver disease effects .
    FXR agonist 14

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