2. Metabolic Enzyme/Protease GPCR/G Protein Apoptosis NF-κB
  3. FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Heme Oxygenase (HO) Quinone Reductase Keap1-Nrf2
  4. FXR agonist 18

FXR 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.

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FXR agonist 18

FXR agonist 18 Chemical Structure

CAS No. : 3061938-00-6

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FXR agonist 18 Related Antibodies

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Description

FXR 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[1].

IC50 & Target[1]

NQO1

 

In Vitro

FXR agonist 18 (Compound 27) potently activates FXR-mediated transcription in HEK-293 cells, with an EC50 of 128 nM[1].
FXR agonist 18 acts as a partial agonist of human MRGPRX4, with an EC50 value of 25,685 nM[1].
FXR agonist 18 (20 μM; 1 h pretreatment, 24 h LPS stimulation) inhibits LPS (HY-D1056)-induced inflammatory responses in RAW264.7 macrophages by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1), upregulating the expression of FXR, Hmox1, Nqo1, and Nrf2, and enhancing antioxidant responses[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FXR agonist 18 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t CL Bioavailability Vss
Rat[1] 10 mg/kg p.o. 2.16 h 0.83 h 3080 ng/mL 11,000 ng·h/mL 931 mL/h/kg 70.30 % /
Rat[1] 2 mg/kg i.v. 1.94 h 0.03 h 12,700 ng/mL 3130 ng·h/mL 683 mL/h/kg / 701 mL/kg
In Vivo

FXR agonist 18 (30 mg/kg; p.o.; once daily; for 4 consecutive weeks) effectively ameliorates CCl4-induced liver fibrosis in mice by restoring parenchymal integrity and inhibiting extracellular matrix accumulation[1].
FXR agonist 18 (20 mg/kg; p.o.; once daily; for 5 consecutive days) exerts significant protective effects in mice with ANIT (HY-W540630)-induced cholestatic liver injury by normalizing serum biomarkers and alleviating hepatocellular damage[1].
At a dose of 20 mg/kg, FXR agonist 18 (10-20 mg/kg; p.o.; daily; 4 weeks) improves histopathological, fibrotic and serum biomarker parameters in a metabolic dysfunction-associated steatohepatitis (MASH) model induced by the combination of Western diet (WD) and CCl4; the 10 mg/kg dose also exhibits significant anti-MASH efficacy[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (8-week-old male, CCl4-induced liver fibrosis)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Markedly attenuated fibrotic pathology, including thinner collagen septa with reduced bridging architecture in portal regions.
Significantly reduced collagen deposition confirmed by Sirius red quantification.
Significantly reduced total liver collagen content compared to the OCA group.
Animal Model: C57BL/6J (8-week-old male, ANIT-induced cholestatic liver injury)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 5 days
Result: Effectively normalized all measured serum biomarkers (ALT, AST, ALP, TBA, TBIL) to levels comparable to normal controls.
Showed near-normal liver histology with minimal necrosis or inflammation.
Significantly reduced histopathological injury scores compared to the ANIT model group.
Animal Model: C57BL/6J (8-week-old male, WD- and CCl4-coinduced metabolic dysfunction-associated steatohepatitis)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; daily; 4 weeks
Result: At 20 mg/kg: Significantly reduced inguinal and epididymal adipose tissue-to-body weight ratios to normal levels.
Achieved more pronounced reduction in hepatic lipid accumulation than OCA.
Significantly improved hepatocyte ballooning (surpassing OCA efficacy).
Achieved >50% reduction in fibrotic collagen area ratio (greater than OCA's 30% reduction).
Markedly ameliorated mitochondrial ultrastructural injuries.
Showed the most substantial improvements in serum biomarkers (ALT, AST, TBA, TC, HDL, LDL) compared to OCA.
At 10 mg/kg: Ameliorated hepatic steatosis and lobular inflammation.
Attenuated liver fibrosis.
Molecular Weight

476.71

Formula

C27H44N2O3S
CAS No.
SMILES

[H][C@@]12C[C@@H](CC[C@@]1([C@]3(CC[C@@]4([C@H](CC[C@]4([C@@]3([C@@H]([C@@H]2CC)O)[H])[H])[C@@H](CCC5=NNC(O5)=S)C)C)[H])C)O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FXR agonist 18 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FXR agonist 183061938-00-6FXR agonist18FXR agonist-18FXRG protein-coupled Bile Acid Receptor 1TNF ReceptorHeme Oxygenase (HO)Quinone ReductaseKeap1-Nrf2NR1H4G-protein coupled receptor 19GPCR19TGR5GPBAR1Tumor Necrosis Factor ReceptorTNFRHeme OxygenaseRXRβRXRαSD ratshuman embryonic kidney cellsTHRβHEK-293 cellsRAW264.7 macrophagesLXRαInhibitorinhibitorinhibit

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