| 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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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
BAR-502 targets both FXR (farnesoid X receptor) and GPBAR1 (G protein-coupled bile acid receptor 1). By activating FXR, it regulates bile acid homeostasis, lipid metabolism, and inflammation. GPBAR1 activation modulates energy expenditure, glucose metabolism, and immune responses. This dual activity makes it a valuable tool for metabolic disease research.
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| ln Vitro |
BAR502 is an alcohol with a truncated side chain that has two substituents in an α configuration on the B ring. While BAR502 can transactivate the nuclear receptor PXR, it is unable to transactivate GR, PPARγ, or LXR at concentrations of 10 μM. BAR502 raises the quantity of cAMP in THP-1 cells and promotes proglucagon mRNA production in GLUTag cells, an enteroendocrine cell line. In HepG2 cells, BAR502 stimulates the expression of OSTα, BSEP, and SHP. BAR502 has a strong affinity for FXR and is particularly effective in attracting SRC-1 coactivators [1].
In vitro, BAR-502 activates FXR and GPBAR1 with IC50 values of 2 μM and 0.4 μM, respectively. Its activity is measured in cell-based assays by quantifying the activation of downstream signaling pathways. It increases the expression of SHP and ABCG5 in the liver and SHP, FGF15, and GLP1 in the intestine. |
| ln Vivo |
In addition to decreasing steatosis, inflammation, and fibrosis scores and hepatic expression of SREPB1c, FAS, PPARγ, CD36, and CYP7A1 mRNA, BAR502 treatment resulted in a 10% reduction in body weight, increased insulin sensitivity, and HDL circulating levels. BAR502 also increases the expression of SHP and ABCG5 in the liver and SHP, FGF15, and GLP1 in the intestine. BAR502 inhibits CCl4-induced liver fibrosis and increases epWAT browning [2]. BAR502 decreased liver damage in a non-obstructive cholestasis model without producing pruritus. Combination therapy with BAR502 increases lifespan, lowers serum alkaline phosphatase levels, and, without producing pruritus, significantly alters liver expression of traditional FXR target genes, such as OSTα, BSEP, SHP, and MDR1 [3].
In vivo, BAR-502 promotes the browning of white adipose tissue and reverses liver steatosis and fibrosis. It protects against liver damage caused by a high-fat diet (HFD). It reduces CCl4-induced liver fibrosis. These effects suggest its potential in treating metabolic and liver diseases. |
| Enzyme Assay |
The in vitro receptor binding assay for BAR-502 involves measuring its affinity and activity at FXR and GPBAR1. This is typically done using cell-based assays where receptor activation is measured by transcriptional activity or downstream signaling. The EC50 or IC50 for each receptor is determined.
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| Cell Assay |
In vitro cellular assays for BAR-502 are performed on cells expressing FXR and GPBAR1. The functional agonism is measured by its ability to activate these receptors. Its effects on gene expression, such as the induction of SHP, FGF15, and GLP1, are measured by qPCR.
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| Animal Protocol |
In vivo animal experiments for BAR-502 are conducted in models of diet-induced obesity, liver steatosis, and fibrosis. The compound is administered, and its effects on body weight, adipose tissue browning, liver histology, and fibrosis are assessed.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of BAR-502 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-502 are not readily available in the public domain, as it is primarily a research compound. Its dual activity on FXR and GPBAR1 suggests a potentially complex safety profile. As with all research chemicals, standard laboratory safety practices should be followed.
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| References |
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| Additional Infomation |
BAR-502 is a research compound used to study the role of FXR and GPBAR1 in metabolic diseases. It is also known as BAR502. It is not an FDA-approved drug and is exclusively for research purposes.
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| Molecular Formula |
C25H44O3
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|---|---|
| Molecular Weight |
392.6151
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| Exact Mass |
392.329
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| CAS # |
1612191-86-2
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| Related CAS # |
1612191-86-2;
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| PubChem CID |
101886309
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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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 |
4
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| Heavy Atom Count |
28
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| Complexity |
564
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O([H])[C@]1([H])[C@]([H])(C([H])([H])C([H])([H])[H])[C@]2([H])C([H])([H])[C@@]([H])(C([H])([H])C([H])([H])[C@]2(C([H])([H])[H])[C@@]2([H])C([H])([H])C([H])([H])[C@]3(C([H])([H])[H])[C@@]([H])([C@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])O[H])C([H])([H])C([H])([H])[C@@]3([H])[C@@]21[H])O[H]
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| InChi Key |
HYCMOIGNYNCMRH-APIYUPOTSA-N
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| InChi Code |
InChI=1S/C25H44O3/c1-5-17-21-14-16(27)8-11-25(21,4)20-9-12-24(3)18(15(2)10-13-26)6-7-19(24)22(20)23(17)28/h15-23,26-28H,5-14H2,1-4H3/t15-,16-,17-,18-,19+,20+,21+,22+,23-,24-,25-/m1/s1
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| Chemical Name |
(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-17-((R)-4-hydroxybutan-2-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol
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| Synonyms |
BAR-502 BAR 502 BAR502.
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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) |
DMF : 50 mg/mL (~127.35 mM)
Ethanol :≥ 50 mg/mL (~127.35 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% 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 25.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2547 mL | 1.2735 mL | 2.5470 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06705998
Conditions:NASHLink: https://clinicaltrials.gov/ct2/show/NCT05203367
Conditions:Non-Alcoholic Fatty Liver DiseaseProducts are for research use only; We do not sell to patients
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