2. Metabolic Enzyme/Protease
  3. FXR
  4. FXR agonist 4

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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FXR agonist 4 Chemical Structure

FXR agonist 4 Chemical Structure

CAS No. : 3025841-47-5

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FXR agonist 4 Related Antibodies

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Description

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)[1].

In Vitro

FXR agonist 4 (10 nM-10 μM) shows FXR agonistic activity with an EC50 value of 1.05 μM in HEK293T cells[1].
FXR agonist 4 (1 nM-10 μM) dose-dependently increarses steroid receptor coactivator (SRC)-2 recruitment with an EC50 value of 1.04 μM[1].
FXR agonist 4 (0.1 nM-10 μM) activates FXR in cells with fatty accumulation[1].
FXR agonist 4 (10-50 μM; 48 h) is not toxic to HepG2 cells[1].

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

FXR agonist 4 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cell line
Concentration: 10, 30 and 50 μM
Incubation Time: 48 hours
Result: Showed no toxic effects to HepG2 cells at the testing dose up to 50 μM.
In Vivo

FXR agonist 4 (100 mg/kg; oral administration, once) improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice[1].

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

Animal Model: High fat diet (HFD)-induced C57BL/6J obese (DIO) mice[1]
Dosage: 100 mg/kg
Administration: Oral administration; 100 mg/kg once
Result: Decreased blood triglyceride, total cholesterol and low-density lipoprotein cholesterol levels of DIO mice after treatment for 3 week. Significantly decreased the serum alanine aminotransferase (ALT) level and promoted cholesterol excretion after treatment for 45 days. Increased the expression of Srebp1c, stearoyl-CoA desaturase 1 (Scd1), fatty acid synthetase (Fasn), Diac ylgycerol Acyltransferase 2 (Dgat2), 3 Hydroxy-3-methylglutaryl Coenzyme A Reductase (Hmgcr) and sterol regulatory element binding protein 2 (Srebp2). Improved insulin sensitivity of DIO mice. Reduced mRNA levels of interleukin 1 beta (Il-1β), Il5, Il6, cluster of differentiation 36 (Cd36), inducible nitric oxide synthase (iNOS) and mouse EGF-like module-containing mucin-like hormone receptor-like 1 (F4/80).
Molecular Weight

373.92

Formula

C21H28ClN3O
CAS No.
SMILES

ClC1=CC(N2CCN(C(C34C[C@@H]5C[C@H](C4)C[C@@H](C5)C3)=O)CC2)=C(N)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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FXR agonist 4 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 43025841-47-5FXR agonist4FXR agonist-4FXRNR1H4XJ034piperazine ringOCANAFLDinsulinhepatic inflammationDIO miceInhibitorinhibitorinhibit

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