FXR

Total: 46
Updated: 2019-06-28 15:55:20
Farnesoid X receptor (FXR) is a nuclear hormone receptor critically involved in the regulation of bile acid homeostasis. It is now recognized that bile acids serve as the natural ligands for FXR. Once activated, FXR in turn induces the expression of another nuclear hormone receptor, small heterodimer partner (SHP). FXR, which is highly expressed in the liver, intestine, kidney, adrenal glands, and adipose tissue, is a master regulator of the synthesis and pleiotropic actions of endogenous bile acids (BAs). FXR activation inhibits BA synthesis and has anti-inflammatory effects in atherosclerosis, inflammatory bowel disease, and experimental cholestasis, whereas TGR5 activation, via cAMP-mediated pathways, reduces proinflammatory cytokine production in macrophages and Kupffer cells.

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Saccharides and Glycosides
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Acids and Aldehydes

Chenodeoxycholic acid

Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

  • CAS Number: 474-25-9
  • MF: C24H40O4
  • MW: 392.572
  • Catalog: FXR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 547.1±25.0 °C at 760 mmHg
  • Melting Point: 165-167 °C(lit.)
  • Flash Point: 298.8±19.7 °C
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T0901317

T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively.

  • CAS Number: 293754-55-9
  • MF: C17H12F9NO3S
  • MW: 481.333
  • Catalog: FXR
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 470.5±55.0 °C at 760 mmHg
  • Melting Point: 116-122° C
  • Flash Point: 238.4±31.5 °C
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Glyco-Obeticholic acid

Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist[1].

  • CAS Number: 863239-60-5
  • MF: C28H47NO5
  • MW: 477.68
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Tauro-Obeticholic acid

Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist[1].

  • CAS Number: 863239-61-6
  • MF: C28H49NO6S
  • MW: 527.76
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Androsterone

Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).

  • CAS Number: 53-41-8
  • MF: C19H30O2
  • MW: 290.440
  • Catalog: FXR
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 413.1±45.0 °C at 760 mmHg
  • Melting Point: 180-185ºC
  • Flash Point: 176.4±21.3 °C
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FXR/TGR5 agonist 1

FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the treatment of fatty liver disease.

  • CAS Number: 2677689-72-2
  • MF: C31H32ClN3O3
  • MW: 530.06
  • Catalog: GPCR19
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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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[1][2][3].

  • CAS Number: 145022-92-0
  • MF: C26H44NNaO7S
  • MW: 537.68
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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DY268

DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM in a time-resolved FRET assay). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM[1].

  • CAS Number: 1609564-75-1
  • MF: C30H32N4O5S
  • MW: 560.664
  • Catalog: FXR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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FXR antagonist 2

FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes[1].

  • CAS Number: 1660153-21-8
  • MF: C22H26Cl2N2O2
  • MW: 421.36
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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BAR502

BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.

  • CAS Number: 1612191-86-2
  • MF: C25H44O3
  • MW: 392.623
  • Catalog: GPCR19
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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LY2562175

LY2562175 is a potent and selective FXR agonist with an EC50 of 193 nM.

  • CAS Number: 1103500-20-4
  • MF: C28H27Cl2N3O4
  • MW: 540.44
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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EDP-305

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[1][2].

  • CAS Number: 1933507-63-1
  • MF: C36H58N2O5S
  • MW: 630.92
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Tropifexor

Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.

  • CAS Number: 1383816-29-2
  • MF: C29H25F4N3O5S
  • MW: 603.594
  • Catalog: FXR
  • Density: 1.55±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 221 °C
  • Flash Point: N/A
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Cilofexor

Cilofexor is a farnesoid X receptor (FXR) agonist.

  • CAS Number: 1418274-28-8
  • MF: C28H22Cl3N3O5
  • MW: 586.850
  • Catalog: FXR
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 855.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 471.2±34.3 °C
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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[1][2].

  • CAS Number: 2260905-08-4
  • MF: C26H44NNaO7S
  • MW: 537.68
  • Catalog: FXR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Sodium chenodeoxycholate

Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

  • CAS Number: 2646-38-0
  • MF: C24H39NaO4
  • MW: 414.55
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 547.1ºC at 760mmHg
  • Melting Point: 298 °C(dec.)
  • Flash Point: 298.8ºC
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