2. GPCR/G Protein Metabolic Enzyme/Protease Autophagy
  3. G protein-coupled Bile Acid Receptor 1 FXR Autophagy
  4. BAR502

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

For research use only. We do not sell to patients.

BAR502 Chemical Structure

BAR502 Chemical Structure

CAS No. : 1612191-86-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 187 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 170 In-stock
10 mg USD 270 In-stock
25 mg USD 540 In-stock
50 mg USD 860 In-stock
100 mg USD 1380 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

BAR502 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

IC50: 2 μM (FXR), 0.4 μM (GPBAR1)[1]
In Vitro

BAR502 is a truncated side chain alcohol with both substituents on ring B in α-configuration. At the concentration of 10 μM, BAR502 fails to transactivate GR, PPARγ, and LXR, respectively, but it transactivates the nuclear receptor PXR. BAR502 is able to induce the expression of pro-glucagon mRNA in GLUTAg cells, an intestinal endocrine cell line, as well as to increase cAMP concentrations in THP-1 cells. BAR502 induces the expression of OSTα, BSEP, and SHP in HepG2 cells. BAR502 shows a very potent activity in the recruitment of SRC-1 coactivator and high affinity to FXR[1].

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

BAR502 Related Antibodies
In Vivo

Treatment with BAR502 causes a 10% reduction of b.w., increases insulin sensitivity and circulating levels of HDL, while reduces steatosis, inflammatory and fibrosis scores and liver expression of SREPB1c, FAS, PPARγ, CD36 and CYP7A1 mRNA. BAR502 increases the expression of SHP and ABCG5 in the liver and SHP, FGF15 and GLP1 in intestine. BAR502 promotes the browning of epWAT and reduces liver fibrosis induced by CCl4[2]. In models of non-obstructive cholestasis, BAR502 attenuates liver injury without causing itching. Co-treatment with BAR502 increases survival, attenuates serum alkaline phosphatase levels and robustly modulates the liver expression of canonical FXR target genes including OSTα, BSEP, SHP and MDR1, without inducing pruritus[3].

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

392.62

Formula

C25H44O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](CCO)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C
Shipping

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

DMF : 50 mg/mL (127.35 mM; Need ultrasonic)

Ethanol : ≥ 50 mg/mL (127.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5470 mL 12.7350 mL 25.4699 mL
5 mM 0.5094 mL 2.5470 mL 5.0940 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.53%

COA (250 KB) RP-HPLC (209 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2]

Mice: C57BL6 mice 24 weeks old are fed a high fat diet containing 60% kj fat and fructose in drinking water (42 g/L) or normal diet (6 mice) for 18 weeks. After 10 weeks of HFD, mice are randomized to receive HFD alone (9 mice) or HFD plus BAR502 (15 mg/kg/day) body weight by gavage (9 mice) for 8 weeks. Mice are housed under controlled temperatures (22 °C) and photoperiods (12:12-hour light/dark cycle), allowed unrestricted access to standard mouse chow and tap water and allowed to acclimate to these conditions for at least 5 days before inclusion in an experiment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMF / Ethanol 1 mM 2.5470 mL 12.7350 mL 25.4699 mL 63.6748 mL
5 mM 0.5094 mL 2.5470 mL 5.0940 mL 12.7350 mL
10 mM 0.2547 mL 1.2735 mL 2.5470 mL 6.3675 mL
15 mM 0.1698 mL 0.8490 mL 1.6980 mL 4.2450 mL
20 mM 0.1273 mL 0.6367 mL 1.2735 mL 3.1837 mL
25 mM 0.1019 mL 0.5094 mL 1.0188 mL 2.5470 mL
30 mM 0.0849 mL 0.4245 mL 0.8490 mL 2.1225 mL
40 mM 0.0637 mL 0.3184 mL 0.6367 mL 1.5919 mL
50 mM 0.0509 mL 0.2547 mL 0.5094 mL 1.2735 mL
60 mM 0.0424 mL 0.2122 mL 0.4245 mL 1.0612 mL
80 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7959 mL
100 mM 0.0255 mL 0.1273 mL 0.2547 mL 0.6367 mL
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BAR502 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:

BAR5021612191-86-2BAR 502BAR-502G protein-coupled Bile Acid Receptor 1FXRAutophagyG-protein coupled receptor 19GPCR19TGR5GPBAR1NR1H4Inhibitorinhibitorinhibit

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