| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GPBAR1 ( EC50 = 1 μM )
BAR-501 targets GPBAR1, a G protein-coupled receptor activated by bile acids. It is a potent and selective agonist with an EC50 of 1 μM. By activating GPBAR1, it exerts genomic and non-genomic effects on CSE, eNOS, and ET-1 in liver sinusoidal cells, leading to vasodilation and reduced portal pressure. |
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| ln Vitro |
BAR501 is a GPBAR1 agonist that is selective and does not agonistically activate FXR. HEK293 cells overexpressing a CRE in addition to GPBAR1 are effectively transactivated by it, with an EC50 of 1 μM. GLP-1 mRNA expression rises by 2.5 times in GLUTAg cells exposed to BAR501 (10 μM)[1].
In vitro, BAR-501 activates GPBAR1 in GPBAR1-overexpressing CRE-HEK293 cells with an EC50 of 1 μM. Its activity is measured in cell-based assays by quantifying the activation of downstream signaling pathways, such as cAMP production. It shows no FXR agonistic activity, confirming its selectivity. |
| ln Vivo |
BAR501, 15 mg/kg, is administered to rats for six days in order to lower basal portal pressure and lessen norepinephrine's vasoconstriction effect. Hepatic vasomotor activity caused by methoxamine and shear stress is reduced when BAR501 is administered beforehand. Giving BAR501 to the CCl4 model causes a direct vasodilatory effect. In mice, portal pressure and AST plasma levels are decreased by BAR501 treatment at a dose of 15 mg/kg. Through the regulation of CSE expression and activity, BAR501 mitigates endothelial dysfunction[1].
In vivo, BAR-501 has been shown to reduce hepatic perfusion pressure and counteract the vasoconstriction activity of norepinephrine in rodent models of portal hypertension. It rescues from endothelial dysfunction. These effects suggest its potential in treating portal hypertension and related liver diseases. |
| Enzyme Assay |
The in vitro receptor binding assay for BAR-501 involves measuring its affinity and activity at GPBAR1. This is typically done using a cell-based assay where GPBAR1 activation is measured by cAMP production. The EC50 for receptor activation is determined.
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| Cell Assay |
HEK-293T cells are plated at 10,000 cells/well in a 24-well plate for GPBAR1-mediated transactivation. The cells are then transfected with 200 ng of pGL4.29, a reporter vector that contains 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. The luciferase activities of HepG2 and HEK293T cells are measured and normalized against the Renilla activities after 18 hours of incubation with 10 μM BAR501 at 24 hours post-transfection[1].
In vitro cellular assays for BAR-501 are performed on cells expressing GPBAR1, such as GPBAR1-overexpressing CRE-HEK293 cells. The functional agonism is measured by its ability to increase cAMP levels. Its effects on downstream signaling pathways, such as eNOS activation, are also studied. |
| Animal Protocol |
Mice: For nine weeks, i.p. 500 μL/Kg body weight of CCl4 in an equivalent volume of paraffin oil is given to C57BL6 mice twice a week. BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water) is randomized to be given to CCL4 mice. Routine biochemical clinical chemistry is used to measure serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase, and alkaline phosphatase[1].
In vivo animal experiments for BAR-501 are conducted in rodent models of portal hypertension. The compound is administered, and its effects on hepatic perfusion pressure, vascular function, and liver fibrosis are assessed. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of BAR-501 are not extensively documented in the available literature. As a small molecule, it is expected to have reasonable oral bioavailability. Its formulation for in vivo studies would typically involve solvents like DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BAR-501 are not readily available in the public domain, as it is primarily a research compound. Its selectivity for GPBAR1 over FXR suggests a potentially favorable safety profile. As with all research chemicals, standard laboratory safety practices should be followed.
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| References | |
| Additional Infomation |
BAR-501 is a research compound used to study the role of GPBAR1 in liver disease, particularly portal hypertension. It is also known as BAR501 and (3α,5β,6β,7β)-6-ethylcholate-3,7,24-triol. It is not an FDA-approved drug and is exclusively for research purposes.
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| Molecular Formula |
C26H46O3
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|---|---|
| Molecular Weight |
406.6416
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| Exact Mass |
406.34
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| Elemental Analysis |
C, 76.79; H, 11.40; O, 11.80
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| CAS # |
1632118-69-4
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| Related CAS # |
1632118-69-4
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| PubChem CID |
101886302
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| Appearance |
White to off-white solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
578
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC[C@H]1[C@@H]2C[C@@H](CC[C@@]2([C@H]3CC[C@]4([C@H]([C@@H]3[C@H]1O)CC[C@@H]4[C@H](C)CCCO)C)C)O
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| InChi Key |
DQBAHTQWQZRMFH-CRPAWOMZSA-N
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| InChi Code |
InChI=1S/C26H46O3/c1-5-18-22-15-17(28)10-12-26(22,4)21-11-13-25(3)19(16(2)7-6-14-27)8-9-20(25)23(21)24(18)29/h16-24,27-29H,5-15H2,1-4H3/t16-,17-,18+,19-,20+,21+,22+,23+,24+,25-,26-/m1/s1
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| Chemical Name |
(3R,5S,6S,7S,8S,9S,10S,13R,14S,17R)-6-ethyl-17-[(2R)-5-hydroxypentan-2-yl]-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol
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| Synonyms |
BAR 501; BAR-501; BAR501
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~123 mM)
Ethanol: ~120 mg/mL (~295.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.38 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (7.38 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix well. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.75 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.75 mg/mL (6.76 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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