FXR
FXR; NR1H4
Farnesoid X receptor (FXR) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. FXR regulates the expression of various genes by binding to DNA either as a monomer or a heterodimer with the common partner for NRs, retinoid x receptor (RXR), to FXR response elements. Two known FXR genes exist, the FXRα and FXRβ.
FXR is mainly expressed in liver and small intestine, where it plays an important role in bile acid, lipid, and glucose metabolism. FXR affects several metabolic pathways through its specific target genes, regulating bile acid (BA) synthesis and homeostasis, glucose and lipid metabolism, also exhibiting a crucial role in intestinal bacterial growth and liver regeneration.
All Product Categories
-
FXR Related Products (183)
Related Products (183)
-
Antibodies (2)
-
Ligusticum cycloprolactam
0 ImagesCat. No.: HY-N17383CAS No.: 2283387-37-9Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.
-
FXR DUBTAC modulator-1
0 ImagesCat. No.: HY-182350CAS No.: 3081876-96-9FXR DUBTAC modulator-1 is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC modulator-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC modulator-1 can be used in the research of cholestatic liver injury.
-
FXR agonist 12
0 ImagesCat. No.: HY-164799CAS No.: 1831862-88-4FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models.
-
Alismanol M
0 ImagesCat. No.: HY-N10640CAS No.: 2408810-59-1Alismanol 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.
-
Glycocholic acid-13C2,d4N
0 ImagesCat. No.: HY-W754548Glycocholic 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).
-
Hyocholic Acid (Standard)
0 ImagesHyocholic Acid (Standard) is the analytical standard of Hyocholic Acid. This product is intended for research and analytical applications. 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 [1][2][3].
-
FXR agonist 18
0 ImagesCat. No.: HY-183692CAS No.: 3061938-00-6FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
-
LZ-007
0 ImagesCat. No.: HY-168713CAS No.: 2920000-23-1LZ-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
-
XJ02862-S2
0 ImagesCat. No.: HY-149971CAS No.: 3023355-55-4XJ02862-S2 shows potent FXR agonistic activity. XJ02862-S2 is a promising lead compound for the research of NAFLD.
-
Teduglutide TFA
0 ImagesCat. No.: HY-P1624ASynonyms: ALX-0600 TFATeduglutide 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.
-
Hyocholic acid-d5
0 ImagesCat. No.: HY-121238S1Hyocholic Acid-d5 is the deuterium labeled Hyocholic Acid.
-
Gly-β-MCA (Standard)
0 ImagesCat. No.: HY-114392RCAS No.: 66225-78-3Gly-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].
-
FXR antagonist 2
0 ImagesCat. No.: HY-148874CAS No.: 1660153-21-8FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes.
-
FXR agonist 13
0 ImagesCat. No.: HY-178959FXR 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).
-
ACT001 hydrochloride
0 ImagesCat. No.: HY-128861BCAS No.: 1403357-80-1Synonyms: Dimethylaminomicheliolide hydrochloride; DMAMCL hydrochlorideACT001 (Dimethylaminomicheliolide; DMAMCL) hydrochloride is an orally active, blood-brain barrier-permeable anti-inflammatory and anti-tumor agent. ACT001 hydrochloride exerts microglia-mediated neuroanti-inflammatory effects by inhibiting the AKT/NF-κB/NLRP3 axis and suppressing apoptosis (apoptosis). ACT001 hydrochloride inhibits tumor proliferation by upregulating NKTR and inhibiting AKT. ACT001 hydrochloride alleviates metabolic-associated fatty liver disease by regulating gut microbiota and inhibiting ileal FXR. ACT001 hydrochloride inhibits pyroptosis (pyroptosis) and pro-inflammatory cytokine release by activating PPAR-γ and inhibiting NF-κB/NLRP3.
-
Ursodeoxycholic acid-13C
0 ImagesCat. No.: HY-13771S1CAS No.: 63296-46-8Synonyms: Ursodeoxycholate-13C; Ursodiol-13C; UDCA-13CUrsodeoxycholic 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.
-
GSK8062
0 ImagesCat. No.: HY-111049CAS No.: 943549-47-1GSK8062 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.
-
2-Oxokolavenol
0 ImagesCat. No.: HY-N1749CAS No.: 130395-82-32-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.
-
Cilofexor tromethamine
0 ImagesCat. No.: HY-109083ACAS No.: 2253764-93-9Synonyms: GS-9674 tromethamineCilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis.
