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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%
BAR502 is a dual FXR and GPBAR1 agonist. BAR-502 promotes browning of white adipose tissue and reverses liver steatosis and fibrosis. BAR502 protects against liver damage caused by HFD by promoting the browning of adipose tissue.
| 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].
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| 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].
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| References |
[1]. Festa C, et al. Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands. J Med Chem. 2014 Oct 23;57(20):8477-95.
[2]. Carino A, et al. BAR502, a dual FXR and GPBAR1 agonist, promotes browning of white adipose tissue and reverses liver steatosis and fibrosis. Sci Rep. 2017 Feb 16;7:42801. [3]. Cipriani S, et al. Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling. PLoS One. 2015 Jul 15;10(7):e0129866 |
| Molecular Formula |
C25H44O3
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|---|---|
| Molecular Weight |
392.624
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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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| SMILES |
O[C@@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)[C@@H]([C@@H](CCO)C)CC[C@@]4([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]2([H])C1
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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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| 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.
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