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BAR502

Catalog No. TQ0252 CAS 1612191-86-2

BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).

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BAR502, CAS 1612191-86-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 107.00
5 mg	In stock	$ 323.00
10 mg	In stock	$ 490.00
25 mg	In stock	$ 783.00
50 mg	In stock	$ 1,090.00
100 mg	In stock	$ 1,480.00

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Purity: 99.91%

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Description	BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
Targets&IC50	FXR:2 μM, GPBAR1:0.4 μM
In vitro	At the concentration of 10 μM, BAR502 fails to transactivate GR, PPARγ, and LXR, respectively, but it transactivates the nuclear receptor PXR. BAR502 is able to induce the expression of proglucagon mRNA in GLUTAg cells, an intestinal endocrine cell line, as well as to increase cAMP concentrations in THP-1 cells. BAR502 induces the expression of OSTα, BSEP, and SHP in HepG2 cells. BAR502 shows very potent activity in the recruitment of SRC-1 coactivator and high affinity to FXR [1].
In vivo	In non-obstructive cholestasis models, BAR502 mitigates liver damage without inducing itching. Concurrently, BAR502 enhances survival, lowers serum alkaline phosphatase levels, and significantly alters the liver's expression of key FXR target genes such as OSTα, BSEP, SHP, and MDR1, without causing pruritus. Furthermore, BAR502 treatment results in a 10% body weight reduction, heightened insulin sensitivity, increased HDL levels, and decreased liver steatosis, inflammation, fibrosis scores, and the expression of liver genes like SREPB1c, FAS, PPARγ, CD36, and CYP7A1 mRNA. It also elevates SHP and ABCG5 expression in the liver, alongside SHP, FGF15, and GLP1 in the intestine. Additionally, BAR502 fosters epWAT browning and curtails CCl4-induced liver fibrosis.
Animal Research	C57BL6 mice 24 weeks old are fed a high-fat diet containing 60% kj fat and fructose in drinking water (42?g/L) or normal diet (6 mice) for 18 weeks. After 10 weeks of HFD, mice are randomized to receive HFD alone (9 mice) or HFD plus BAR502 (15?mg/kg/day) body weight by gavage (9 mice) for 8 weeks. Mice are housed under controlled temperatures (22?°C) and photoperiods (12:12-hour light/dark cycle), allowed unrestricted access to standard mouse chow and tap water and allowed to acclimate to these conditions for at least 5 days before inclusion in an experiment [3].

Molecular Weight	392.62
Formula	C25H44O3
CAS No.	1612191-86-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMF: 48 mg/mL (122.26 mM), Sonication is recommended.

References and Literature

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. 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. 3. 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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Metabolism Compound Library Anti-Cancer Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Bioactive Compound Library Immunology/Inflammation Compound Library Lipid Metabolism Compound Library Nuclear Receptor Compound Library NO PAINS Compound Library

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Keywords

BAR502 1612191-86-2 Autophagy GPCR/G Protein Metabolism FXR GPCR19 G protein-coupled Bile Acid Receptor 1 GPBAR1 BAR-502 NR1H4 Inhibitor G-protein coupled receptor 19 inhibit BAR 502 TGR5 inhibitor

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