1. GPCR/G Protein
  2. GPCR19
  3. BAR501

BAR501 

Cat. No.: HY-101274 Purity: >98.0%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 140 In-stock
Estimated Time of Arrival: December 31
1 mg USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 276 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2160 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
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Description

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

IC50 & Target

EC50: 1 μM (GPBAR1)[1]

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].

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

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].

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

Molecular Weight

406.64

Formula

C₂₆H₄₆O₃

CAS No.

1632118-69-4

SMILES
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: 

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

DMSO : ≥ 50 mg/mL (122.96 mM)

*"≥" 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
10 mM 0.2459 mL 1.2296 mL 2.4592 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (6.76 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (6.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (6.76 mM); Clear solution

  • 4.

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

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

  • 5.

    Add each solvent one by one:  10% EtOH    90% corn oil

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

*All of the co-solvents are provided by MCE.
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
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Keywords:

BAR501BAR 501BAR-501GPCR19G-protein coupled receptor 19Inhibitorinhibitorinhibit

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BAR501
Cat. No.:
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