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FXR activators

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64

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1

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4

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12

Isotope-Labeled Compounds

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15371
    Forskolin
    Maximum Cited Publications
    210 Publications Verification

    Coleonol; Colforsin; HL 362

    Organoid Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
    Forskolin
  • HY-76847
    Chenodeoxycholic Acid
    20+ Cited Publications

    CDCA

    FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid
  • HY-13771
    Ursodeoxycholic acid
    25+ Cited Publications

    Ursodeoxycholate; Ursodiol; UDCA

    G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Infection Metabolic Disease Cancer
    Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active .
    Ursodeoxycholic 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-107859
    Tris(2-chloroethyl) phosphate
    5+ Cited Publications

    TCEP

    Environmental Pollutants Apoptosis FXR Calcium Channel Toll-like Receptor (TLR) SOD Reactive Oxygen Species (ROS) DNA/RNA Synthesis Interleukin Related NF-κB TNF Receptor Others
    Tris(2-chloroethyl) phosphate (TCEP) is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation .
    Tris(2-chloroethyl) phosphate
  • HY-107738
    Guggulsterone
    20+ Cited Publications

    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-P1624
    Teduglutide
    2 Publications Verification

    ALX-0600

    Nuclear Hormone Receptor 4A/NR4A FXR Inflammation/Immunology
    Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
    Teduglutide
  • HY-76847S
    Chenodeoxycholic Acid-d4
    1 Publications Verification

    CDCA-d4

    FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d4
  • HY-121238
    Hyocholic acid
    2 Publications Verification

    FXR G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes .
    Hyocholic acid
  • HY-N0010
    Geniposidic acid
    5+ Cited Publications

    FXR Sirtuin TNF Receptor Interleukin Related Metabolic Disease
    Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis .
    Geniposidic acid
  • 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-13771A
    Ursodeoxycholic acid sodium
    25+ Cited Publications

    Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium

    G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite Metabolic Disease Inflammation/Immunology Cancer
    Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .
    Ursodeoxycholic acid sodium
  • HY-N0468
    Rebaudioside D
    1 Publications Verification

    FXR Acetyl-CoA Carboxylase Metabolic Disease
    Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D
  • 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-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-113478S

    Ursodeoxycholate-d4; Ursodiol-d4; UDCA-d4

    Isotope-Labeled Compounds Infection Metabolic Disease
    Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection .
    Ursodeoxycholic acid-d4
  • HY-N0805
    Alisol B 23-acetate
    3 Publications Verification

    23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate

    Apoptosis Reactive Oxygen Species (ROS) CDK MMP PARP FXR Syk Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma .
    Alisol B 23-acetate
  • HY-76847A
    Chenodeoxycholic acid sodium
    20+ Cited Publications

    CDCA sodium

    FXR Autophagy Endogenous Metabolite Metabolic Disease Cancer
    Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid sodium
  • HY-76847R
    Chenodeoxycholic Acid (Standard)
    20+ Cited Publications

    CDCA (Standard)

    Reference Standards FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid (Standard) is the analytical standard of Chenodeoxycholic Acid. This product is intended for research and analytical applications. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic 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-N6987

    FXR Factor Xa Cardiovascular Disease Inflammation/Immunology
    Licraside, found in Glycyrrhiza glabra, is a Farnesoid X receptor (FXR) activator. Licraside activates FXR to induce upregulation of SHP and BSEP, regulates bile acid homeostasis, reduces elevated biliary and serum TBA, serum ALT, AST, GGT, ALP, and TBIL levels, and attenuates liver histopathological damage. Licraside inhibits factor Xa with an IC50 of 48.54 mM. Licraside can be used for the research of cholestasis and thromboembolic diseases .
    Licraside
  • HY-15371R

    Coleonol (Standard); Colforsin (Standard); HL 362 (Standard)

    Organoid Reference Standards Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin is also an inducer of intracellular cAMP formation . Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy .
    Forskolin (Standard)
  • HY-W585876

    FXR Metabolic Disease
    Chenodeoxycholic acid 3-glucuronide is a metabolite of Chenodeoxycholic acid that can activate the key nuclear receptor (FXR), with an EC50 of 8 μM, and in HEK293T cells, the EC50 for activating FXR is 11 μM .
    Chenodeoxycholic acid 3-glucuronide
  • HY-N7781

    (E)-Guggulsterone

    FXR Keap1-Nrf2 Heme Oxygenase (HO) Dengue Virus Bacterial Reactive Oxygen Species (ROS) Estrogen Receptor/ERR Cytochrome P450 Drug Metabolite Infection Metabolic Disease Endocrinology
    (-)-(E)-Guggulsterone ((E)-Guggulsterone) is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats .
    (-)-(E)-Guggulsterone
  • 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-151481

    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-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-13771R

    Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)

    Reference Standards G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Infection Metabolic Disease Cancer
    Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active .
    Ursodeoxycholic acid (Standard)
  • HY-76847S3

    CDCA-d5

    Isotope-Labeled Compounds FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-d5
  • HY-76847S2

    CDCA-13C

    FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic acid- 13C is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-13C
  • HY-15371G

    Coleonol; Colforsin; HL 362

    Adenylate Cyclase FXR Autophagy PKC Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase . Forskolin (GMP) is also an inducer of intracellular cAMP formation . Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR . Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy .
    Forskolin
  • HY-W020788

    CGA 154281

    Environmental Pollutants Glutathione S-transferase Estrogen Receptor/ERR Pregnane X Receptor (PXR) FXR Metabolic Disease Cancer
    Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity .
    Benoxacor
  • HY-107859S

    TCEP-d12

    Isotope-Labeled Compounds Reactive Oxygen Species (ROS) Apoptosis DNA/RNA Synthesis Calcium Channel FXR Toll-like Receptor (TLR) NF-κB SOD Interleukin Related TNF Receptor Others
    Tris(2-chloroethyl)phosphate-d12 is the deuterium labeled Tris(β-chloroethyl) phosphate. Tris(2-chloroethyl) phosphate is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.
    Tris(2-chloroethyl)phosphate-d12
  • HY-P1624S1

    ALX-0600-Leu(13C6,15N) sodium

    Isotope-Labeled Compounds Nuclear Hormone Receptor 4A/NR4A FXR Inflammation/Immunology
    Teduglutide-Leu( 13C6, 15N) (ALX-0600-Leu( 13C6, 15N)) sodium is the 13C- and 15N-labeled Teduglutide (HY-P1624). Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
    Teduglutide-Leu(13C6,15N) sodium
  • HY-76847S1

    CDCA-d9

    Isotope-Labeled Compounds FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d9
  • 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-13771S1

    Ursodeoxycholate-13C; Ursodiol-13C; UDCA-13C

    Isotope-Labeled Compounds G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite Cancer
    Ursodeoxycholic acid- 13C is the 13C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .
    Ursodeoxycholic acid-13C
  • HY-P1624A

    ALX-0600 TFA

    Nuclear Hormone Receptor 4A/NR4A FXR Inflammation/Immunology
    Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
    Teduglutide TFA
  • 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-W020788R

    CGA 154281 (Standard)

    Reference Standards Glutathione S-transferase Estrogen Receptor/ERR Pregnane X Receptor (PXR) FXR Others
    Benoxacor (Standard) is the analytical standard of Benoxacor. This product is intended for research and analytical applications. Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity .
    Benoxacor (Standard)
  • HY-107738R

    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-N0468R

    Reference Standards Acetyl-CoA Carboxylase FXR Metabolic Disease
    Rebaudioside D (Standard) is the analytical standard of Rebaudioside D. This product is intended for research and analytical applications. Rebaudioside D is an orally active sweetener that targets and activates FXR, modulates Acetyl-CoA Carboxylase, and inhibits 3-hydroxy-3-methylglutaryl-CoA reductase. Rebaudioside D regulates bile acid homeostasis and lipid metabolism, reduces the synthesis rates of fatty acids and cholesterol, and exerts multiple effects including anti-adipogenesis, hepatoprotection, anti-steatosis, gut microbiota modulation, enhancement of secondary bile acid metabolism, anti-endotoxin activity, regulation of bile acid transport, and inhibition of bile acid efflux. Rebaudioside D also reduces body weight gain, visceral fat accumulation, hepatic triglyceride and cholesterol accumulation, hepatic lipid peroxidation, and decreases the circulating level of lipopolysaccharide-binding protein. Rebaudioside D additionally enhances the secondary bile acid metabolic pathway of intestinal bacteria, upregulates the gene expression of ileal organic solute transporter α, and downregulates the gene expression of hepatic bile salt export pump. Rebaudioside D does not affect glucose homeostasis, alter total caloric intake or fecal energy excretion, induce weight gain, exacerbate obesity, promote hepatic steatosis, impair brown adipose tissue function, nor change skeletal muscle metabolism-related proteins. Rebaudioside D can be used in diet-induced obesity and obesity-related research .
    Rebaudioside D (Standard)
  • HY-168516

    FXR Others
    FXR/CES2 modulator 1 (compound LE-77) is a doul modulator that activates FXR and inhibits CES2. FXR/CES2 modulator 1 effectively mitigates the intestinal toxicity of irinotecan .
    FXR/CES2 modulator 1
  • 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-N15305

    FXR Inflammation/Immunology
    Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
    Ferolin
  • HY-133969

    FXR Metabolic Disease
    5β-Cholane is a farnesoid X receptor (FXR) activator. 5β-Cholane can be used for the research of cholesterol and lipid-related diseases .
    5β-Cholane
  • HY-135221R

    Reference Standards Bacterial Antibiotic Infection
    Chenodeoxycholic Acid (Standard) is the analytical standard of Chenodeoxycholic Acid. This product is intended for research and analytical applications. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Cefcapene pivoxil hydrochloride (Standard)
  • HY-76847S4

    CDCA-d2

    Isotope-Labeled Compounds Endogenous Metabolite FXR Autophagy Metabolic Disease Cancer
    Chenodeoxycholic acid-d2 (CDCA-d2) is deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-d2
  • HY-W712932

    CDCA-d7

    Isotope-Labeled Compounds FXR Autophagy Endogenous Metabolite Metabolic Disease
    Chenodeoxycholic Acid-d7 (CDCA-d7) is the deuterium labeled Chenodeoxycholic Acid (HY-76847). Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d7
  • HY-133890AS

    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

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