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

FXR agonist 4 Chemical Structure

CAS No. : 3025841-47-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

Off-white to light brown

SMILES

ClC1=CC(N2CCN(C(C34C[C@@H]5C[C@H](C4)C[C@@H](C5)C3)=O)CC2)=C(N)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (267.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6744 mL 13.3718 mL 26.7437 mL
5 mM 0.5349 mL 2.6744 mL 5.3487 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6744 mL 13.3718 mL 26.7437 mL 66.8592 mL
5 mM 0.5349 mL 2.6744 mL 5.3487 mL 13.3718 mL
10 mM 0.2674 mL 1.3372 mL 2.6744 mL 6.6859 mL
15 mM 0.1783 mL 0.8915 mL 1.7829 mL 4.4573 mL
20 mM 0.1337 mL 0.6686 mL 1.3372 mL 3.3430 mL
25 mM 0.1070 mL 0.5349 mL 1.0697 mL 2.6744 mL
30 mM 0.0891 mL 0.4457 mL 0.8915 mL 2.2286 mL
40 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6715 mL
50 mM 0.0535 mL 0.2674 mL 0.5349 mL 1.3372 mL
60 mM 0.0446 mL 0.2229 mL 0.4457 mL 1.1143 mL
80 mM 0.0334 mL 0.1671 mL 0.3343 mL 0.8357 mL
100 mM 0.0267 mL 0.1337 mL 0.2674 mL 0.6686 mL
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FXR agonist 4 Related Classifications

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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