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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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Purity: ≥98%
BAR-501 is a selective GPBAR1 agonist devoid of any FXR agonistic activity. BAR501 successfully countered norepinephrine's vasoconstriction action and lowered the hepatic perfusion pressure. BAR501 demonstrates both genomic and non-genomic effects on CSE, eNOS, and ET-1 in liver sinusoidal cells, thereby providing rescue from endothelial dysfunction in rodent models of portal hypertension.
| Targets |
GPBAR1 ( EC50 = 1 μM )
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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].
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| 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].
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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].
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| 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].
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| References |
| 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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