Search Result
Results for "
FXR receptor
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
21
Isotope-Labeled Compounds
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-15371
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Forskolin
Maximum Cited Publications
210 Publications Verification
Coleonol; Colforsin; HL 362
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Organoid
Adenylate Cyclase
FXR
Autophagy
PKC
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Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
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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 .
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- HY-76847
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- HY-13771
-
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Ursodeoxycholate; Ursodiol; UDCA
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G protein-coupled Bile Acid Receptor 1
FXR
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
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Infection
Metabolic Disease
Cancer
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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 .
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- HY-N1423
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P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Endogenous Metabolite
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
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Metabolic Disease
Inflammation/Immunology
Cancer
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Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
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- HY-10626
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LXR
FXR
ROR
Apoptosis
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Cardiovascular Disease
Metabolic Disease
Cancer
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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 .
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- HY-114392
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FXR
Autophagy
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Metabolic Disease
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Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders .
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- HY-107738
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Z/E-Guggulsterone
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Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
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Cancer
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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 .
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- HY-135103
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T-βMCA sodium
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FXR
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Cancer
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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 .
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- HY-10912
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FXR
Autophagy
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Others
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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 .
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- HY-P1624
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ALX-0600
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Nuclear Hormone Receptor 4A/NR4A
FXR
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Inflammation/Immunology
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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 .
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- HY-110267
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DY268
3 Publications Verification
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FXR
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Metabolic Disease
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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) .
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- HY-76847S
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- HY-13771A
-
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Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium
|
G protein-coupled Bile Acid Receptor 1
FXR
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
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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 .
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- HY-14908
-
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4sc-101; SC12267
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Dihydroorotate Dehydrogenase
Interleukin Related
FXR
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Infection
Inflammation/Immunology
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Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR .
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- HY-N1423A
-
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P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
Endogenous Metabolite
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Metabolic Disease
Cancer
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Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
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- HY-N1423S
-
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Isotope-Labeled Compounds
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Endogenous Metabolite
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
|
Metabolic Disease
Cancer
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Glycocholic acid-d4 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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- HY-113478S
-
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Ursodeoxycholate-d4; Ursodiol-d4; UDCA-d4
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Isotope-Labeled Compounds
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Infection
Metabolic Disease
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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 .
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- HY-76847A
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- HY-76847R
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CDCA (Standard)
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Reference Standards
FXR
Endogenous Metabolite
Autophagy
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Metabolic Disease
Cancer
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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.
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- HY-12434
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-
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- HY-N3431
-
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AMPK
PD-1/PD-L1
FXR
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
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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 .
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- HY-134988
-
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FXR
Phosphatase
Cytochrome P450
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Inflammation/Immunology
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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 .
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- HY-109096
-
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LMB763
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FXR
Autophagy
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Inflammation/Immunology
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Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH) .
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- HY-N6987
-
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FXR
Factor Xa
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Cardiovascular Disease
Inflammation/Immunology
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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 .
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- HY-100277
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SR-202
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PPAR
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Metabolic Disease
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Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
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- HY-15371R
-
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Coleonol (Standard); Colforsin (Standard); HL 362 (Standard)
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Organoid
Reference Standards
Adenylate Cyclase
FXR
Autophagy
PKC
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Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-W013105
-
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N-Cholylglycine sodium salt, 98%
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Bcl-2 Family
Caspase
Endogenous Metabolite
Bacterial
MDM-2/p53
P-glycoprotein
LPL Receptor
FXR
G protein-coupled Bile Acid Receptor 1
Apoptosis
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Others
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Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
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- HY-N7781
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-
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- HY-N0910
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-
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- HY-W585876
-
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FXR
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Metabolic Disease
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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 .
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- HY-13771R
-
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Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)
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Reference Standards
G protein-coupled Bile Acid Receptor 1
FXR
Angiotensin-converting Enzyme (ACE)
Endogenous Metabolite
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Infection
Metabolic Disease
Cancer
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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 .
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- HY-N1423B
-
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Endogenous Metabolite
Caspase
G protein-coupled Bile Acid Receptor 1
LPL Receptor
MDM-2/p53
Bcl-2 Family
P-glycoprotein
FXR
Bacterial
Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
|
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Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
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- HY-76847S3
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- HY-76847S2
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- HY-169792
-
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FXR
Aminotransferases (Transaminases)
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Metabolic Disease
Inflammation/Immunology
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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) .
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- HY-15371G
-
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Coleonol; Colforsin; HL 362
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Adenylate Cyclase
FXR
Autophagy
PKC
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Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
|
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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 .
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- HY-163436
-
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FXR
Cytochrome P450
RAR/RXR
PPAR
ROR
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Metabolic Disease
|
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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 .
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- HY-151959
-
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FXR
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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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) .
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- HY-135399
-
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FXR
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Inflammation/Immunology
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Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-N3209
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-
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- HY-P1624S1
-
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ALX-0600-Leu(13C6,15N) sodium
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Isotope-Labeled Compounds
Nuclear Hormone Receptor 4A/NR4A
FXR
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Inflammation/Immunology
|
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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 .
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- HY-100443
-
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PX-102
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FXR
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Cancer
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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 .
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- HY-W587537
-
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FXR
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Metabolic Disease
|
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Deoxycholic Acid 3-O-beta-D-Glucuronide disodium salt is a bile acid receptor (FXR) agonist.
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- HY-76847S1
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- HY-14908A
-
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4sc-101 hemicalcium; SC12267 hemicalcium
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Dihydroorotate Dehydrogenase
Interleukin Related
FXR
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Infection
Inflammation/Immunology
|
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Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR .
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- HY-N10640
-
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FXR
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Inflammation/Immunology
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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 .
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- HY-W587451
-
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OCA-3-glucuronide disodium
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FXR
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Metabolic Disease
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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 .
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- HY-13771S1
-
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Ursodeoxycholate-13C; Ursodiol-13C; UDCA-13C
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Isotope-Labeled Compounds
G protein-coupled Bile Acid Receptor 1
FXR
Endogenous Metabolite
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Cancer
|
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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 .
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- HY-B1734
-
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16-DPA
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FXR
5 alpha Reductase
Cytochrome P450
Drug Intermediate
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Cardiovascular Disease
Cancer
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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 .
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- HY-153114
-
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FXR
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Inflammation/Immunology
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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 .
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- HY-10626R
-
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Reference Standards
LXR
FXR
ROR
Apoptosis
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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 .
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- HY-P1624A
-
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ALX-0600 TFA
|
Nuclear Hormone Receptor 4A/NR4A
FXR
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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 .
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- HY-N1423S1
-
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Isotope-Labeled Compounds
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Endogenous Metabolite
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
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Metabolic Disease
Cancer
|
|
Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
|
-
- 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.
|
-
- HY-163072
-
|
|
FXR
|
Metabolic Disease
|
|
FXR antagonist 3 (V02-8) is an intestine-specific farnesoid X receptor (FXR) antagonist, with an IC50 of 0.89 μM .
|
-
- HY-159845
-
-
- 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) .
|
-
- 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 .
|
-
- HY-135400
-
|
|
FXR
|
Inflammation/Immunology
|
|
Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
|
-
- 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 .
|
-
- HY-121110
-
|
|
FXR
|
Metabolic Disease
|
|
Fexarene is a potent and selective nonsteroidal Farnesoid X Receptor (FXR) agonist with an EC50 of 36 nM. Fexarene can be used in studies of cholesterol and bile acid metabolism .
|
-
- 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 .
|
-
- 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.
|
-
- HY-135400S
-
|
|
FXR
|
Inflammation/Immunology
|
|
Glyco-obeticholic acid-d5 is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
|
-
- HY-76847S4
-
-
- HY-111049
-
|
|
FXR
|
Metabolic Disease
|
|
GSK8062 is a farnesoid X receptor (FXR) agonist with activity that improves compound development parameters. Analog 1c of GSK8062 showed a reduction in weight gain and serum glucose levels .
|
-
- HY-W712932
-
-
- HY-12365S2
-
-
- HY-135399S
-
-
- HY-W653920
-
|
|
Isotope-Labeled Compounds
FXR
|
Inflammation/Immunology
|
|
Tauro 6-ethlchenodeoxycholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
|
-
- HY-135103S
-
|
|
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 .
|
-
- HY-139562
-
|
|
FXR
|
Metabolic Disease
|
|
BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-114392R
-
|
|
Reference Standards
FXR
Autophagy
|
Metabolic Disease
|
|
Gly-β-MCA (Standard) is the analytical standard of Gly-β-MCA. This product is intended for research and analytical applications. Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
|
-
- HY-10912R
-
|
|
FXR
Autophagy
|
Others
|
|
Fexaramine (Standard) is the analytical standard of Fexaramine. This product is intended for research and analytical applications. 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 .
|
-
- HY-W654353
-
|
T-α-MCA-d4-1 sodium
|
Isotope-Labeled Compounds
FXR
Endogenous Metabolite
|
Others
|
|
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
|
-
- HY-168713
-
|
|
FXR
|
Metabolic Disease
|
|
LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
|
-
- HY-100277R
-
|
SR-202 (Standard)
|
Reference Standards
PPAR
|
Metabolic Disease
|
|
Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-N7781R
-
-
- HY-N1423AR
-
|
|
Reference Standards
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
|
-
- HY-W754548
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
|
Metabolic Disease
Cancer
|
|
Glycocholic acid- 13C2,d4 is the deuterium labeled and 13C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
|
-
- HY-P1624S
-
|
ALX-0600-Ala(13C3,15N) sodium
|
Isotope-Labeled Compounds
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide-Ala( 13C3, 15N) (ALX-0600-Ala( 13C3, 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 .
|
-
- HY-183309
-
|
|
FXR
17β-HSD
|
Inflammation/Immunology
|
|
FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis .
|
-
- HY-179703
-
|
|
FXR
|
Inflammation/Immunology
|
|
FXR agonist 15 is a selective, potent and orally active farnesoid X receptor (FXR) agonist with EC50 of 0.76 μM. FXR agonist 15 exhibits no obvious activation on other nuclear receptors including LXRα/β, PXR, PPARα/β/γ, THR-β, with EC50 values all >10 μM. FXR agonist 15 can alleviate steatosis, lobular inflammation, hepatocyte ballooning and liver fibrosis. FXR agonist 15 can be used for the research of nonalcoholic steatohepatitis (NASH) .
|
-
- HY-181102
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
Inflammation/Immunology
|
|
TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes .
|
-
- HY-N1749
-
|
|
FXR
|
Others
|
|
2-Oxokolavenol is a selective agonist targeting the farnesoid X receptor (FXR), with an EC50 of ~3.7 μM. 2-Oxokolavenol exerts its activity against Acetaminophen (HY-66005)-induced hepatocyte damage in an FXR-dependent manner by binding to the FXR ligand-binding pocket, recruiting co-activators, and inducing FXR transcriptional activity. 2-Oxokolavenol can be naturally extracted from Aglaia spectabilis (a plant of the Aglaia genus in the Meliaceae family) and can be used in research related to liver diseases .
|
-
- HY-182395
-
|
|
FXR
|
Others
|
|
DM175 is a partial agonist of FXR. DM175 binds to the ligand-binding domain of FXR and induces the outward movement of Trp454 .
|
-
- HY-41333
-
-
- HY-135400S2
-
|
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Glyco-obeticholic acid-d4 is the deuterium labeled Glyco-obeticholic acid (HY-135400). Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
|
-
- HY-135399S2
-
|
|
Isotope-Labeled Compounds
FXR
|
Inflammation/Immunology
|
|
Tauro-obeticholic acid-d4 is the deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
|
-
- HY-181876
-
|
|
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 .
|
-
- HY-176961
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
Homocholic acid is a synthetic steroid analogue. Homocholic acid can be labeled with 75Se and is used for SeHCAT detection (a method for diagnosing bile acid malabsorption) .
|
-
-
- HY-15371G
-
|
Coleonol; Colforsin; HL 362
|
Fluorescent Dyes
|
|
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 .
|
-
- HY-W013105
-
|
N-Cholylglycine sodium salt, 98%
|
Biochemical Assay Reagents
|
|
Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
|
-
- HY-15371G
-
|
Coleonol; Colforsin; HL 362
|
Biochemical Assay Reagents
|
|
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 .
|
| Cat. No. |
상품명 |
Target |
Research Area |
-
- HY-P1624
-
|
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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-P1624S
-
|
ALX-0600-Ala(13C3,15N) sodium
|
Isotope-Labeled Compounds
Nuclear Hormone Receptor 4A/NR4A
FXR
|
Inflammation/Immunology
|
|
Teduglutide-Ala( 13C3, 15N) (ALX-0600-Ala( 13C3, 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 .
|
| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
-
- HY-15371
-
-
-
- HY-76847
-
-
-
- HY-13771
-
-
-
- HY-N1423
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Steroids
Source Classification
Cancer
|
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Endogenous Metabolite
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
|
|
Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
|
-
-
- HY-107738
-
|
Z/E-Guggulsterone
|
Triterpenes
Structural Classification
Classification of Application Fields
Terpenoids
Plants
Burseraceae
Disease Research Fields
Commiphora wightii
Cancer
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
|
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 .
|
-
-
- HY-13771A
-
-
-
- HY-N1423A
-
|
|
Triterpenes
Structural Classification
Terpenoids
Endogenous metabolite
Source Classification
|
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
Endogenous Metabolite
|
|
Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
|
-
-
- HY-76847A
-
-
-
- HY-76847R
-
-
-
- HY-N3431
-
-
-
- HY-N6987
-
|
|
Structural Classification
Chalcones
Flavonoids
Classification of Application Fields
Leguminosae
Phenols
Polyphenols
Plants
Glycyrrhiza uralensis Fisch.
Inflammation/Immunology
Disease Research Fields
Source Classification
|
FXR
Factor Xa
|
|
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 .
|
-
-
- HY-15371R
-
-
-
- HY-N7781
-
-
-
- HY-N0910
-
-
-
- HY-13771R
-
-
-
- HY-N1423B
-
|
|
Structural Classification
Classification of Application Fields
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Steroids
Source Classification
|
Endogenous Metabolite
Caspase
G protein-coupled Bile Acid Receptor 1
LPL Receptor
MDM-2/p53
Bcl-2 Family
P-glycoprotein
FXR
Bacterial
Apoptosis
|
|
Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA) .
|
-
-
- HY-N3209
-
-
-
- HY-N10640
-
-
-
- HY-107738R
-
|
Z/E-Guggulsterone (Standard)
|
Triterpenes
Structural Classification
Terpenoids
Plants
Burseraceae
Commiphora wightii
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
Reference Standards
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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.
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- HY-N15305
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- HY-N7781R
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- HY-N1423AR
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Structural Classification
Endogenous metabolite
Steroids
Source Classification
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Reference Standards
P-glycoprotein
Bcl-2 Family
G protein-coupled Bile Acid Receptor 1
Bacterial
Apoptosis
FXR
Caspase
MDM-2/p53
LPL Receptor
Endogenous Metabolite
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Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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- HY-N1749
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| Cat. No. |
상품명 |
Chemical Structure |
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- HY-76847S
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1 Publications Verification
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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.
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- HY-N1423S
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Glycocholic acid-d4 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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- HY-113478S
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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 .
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- HY-76847S3
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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.
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- HY-76847S2
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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.
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- HY-P1624S1
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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 .
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- HY-76847S1
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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.
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- HY-13771S1
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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 .
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- HY-N1423S1
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Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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- HY-135400S
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Glyco-obeticholic acid-d5 is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-76847S4
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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.
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- HY-W712932
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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.
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- HY-12365S2
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Tauro-obeticholic acid-d5 is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-135399S
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Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid sodium (HY-135399A). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-W653920
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Tauro 6-ethlchenodeoxycholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-135103S
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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 .
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- HY-W654353
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Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
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- HY-W754548
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Glycocholic acid- 13C2,d4 is the deuterium labeled and 13C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
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- HY-P1624S
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Teduglutide-Ala( 13C3, 15N) (ALX-0600-Ala( 13C3, 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 .
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- HY-135400S2
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Glyco-obeticholic acid-d4 is the deuterium labeled Glyco-obeticholic acid (HY-135400). Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-135399S2
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Tauro-obeticholic acid-d4 is the deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-15371G
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Coleonol; Colforsin; HL 362
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Adenylate Cyclase
FXR
Autophagy
PKC
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Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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