2. GPCR/G Protein
  3. G protein-coupled Bile Acid Receptor 1
  4. BAR501

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

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

BAR501 Chemical Structure

BAR501 Chemical Structure

CAS No. : 1632118-69-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 140 In-stock
Solution
10 mM * 1 mL in DMSO USD 140 In-stock
Solid
5 mg USD 128 In-stock
10 mg USD 200 In-stock
25 mg USD 380 In-stock
50 mg USD 570 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BAR501:

BAR501 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BAR501

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BAR501 is a potent and selective agonist of GPBAR1 with an EC50 of 1 μM.

IC50 & Target

EC50: 1 μM (GPBAR1)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
1.03 μM
Compound: 26, EUDCOH
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay
[PMID: 25247751]
In Vitro

BAR501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC50 of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds[1].

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

BAR501 Related Antibodies
In Vivo

Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity[1].

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

406.64

Formula

C26H46O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](CCCO)[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: 

Ethanol : 120 mg/mL (295.10 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (122.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4592 mL 12.2959 mL 24.5918 mL
5 mM 0.4918 mL 2.4592 mL 4.9184 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (7.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 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.
  • Protocol 2

    Add each solvent one by one:  10% EtOH    90% Corn Oil

    Solubility: ≥ 3 mg/mL (7.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate and transfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drives the transcription of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, and with 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 μM BAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: C57BL6 mice are administered i.p. 500 μL/Kg body weight of CCl4 in an equal volume of paraffin oil twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase are measured by routine biochemical clinical chemistry[1].

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
DMSO / Ethanol 1 mM 2.4592 mL 12.2959 mL 24.5918 mL 61.4794 mL
5 mM 0.4918 mL 2.4592 mL 4.9184 mL 12.2959 mL
10 mM 0.2459 mL 1.2296 mL 2.4592 mL 6.1479 mL
15 mM 0.1639 mL 0.8197 mL 1.6395 mL 4.0986 mL
20 mM 0.1230 mL 0.6148 mL 1.2296 mL 3.0740 mL
25 mM 0.0984 mL 0.4918 mL 0.9837 mL 2.4592 mL
30 mM 0.0820 mL 0.4099 mL 0.8197 mL 2.0493 mL
40 mM 0.0615 mL 0.3074 mL 0.6148 mL 1.5370 mL
50 mM 0.0492 mL 0.2459 mL 0.4918 mL 1.2296 mL
60 mM 0.0410 mL 0.2049 mL 0.4099 mL 1.0247 mL
80 mM 0.0307 mL 0.1537 mL 0.3074 mL 0.7685 mL
100 mM 0.0246 mL 0.1230 mL 0.2459 mL 0.6148 mL
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BAR501 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:

BAR5011632118-69-4BAR 501BAR-501G protein-coupled Bile Acid Receptor 1G-protein coupled receptor 19GPCR19TGR5GPBAR1Inhibitorinhibitorinhibit

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