BAR502

SKU: orb1296098

Description

BAR502 is a dual agonist targeting both the GPBAR1 (TGR5) and FXR receptors, with respective IC50 values of 0.4 μM and 2 μM. This small molecule is a valuable research tool for investigating metabolic and inflammatory pathways in both in vitro and in vivo models of liver and intestinal diseases.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1612191-86-2
MW	392.62
Purity	99.95% (May vary between batches)
Formula	C₂₅H₄₄O₃
SMILES	CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCO)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12
Target	Autophagy,FXR,GPCR19
Solubility	DMF:48 mg/mL (122.26 mM)

Bioactivity

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Target IC50	GPBAR1:0.4 μM\|FXR:2 μM
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. Read more...
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 . Read more...
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 . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BAR 502, BAR502, BAR-502, Autophagy, G-protein coupled receptor 19, GPBAR1, GPCR19, FXR, G protein-coupled Bile Acid Receptor 1, Inhibitor, NR1H4, inhibit, TGR5

Quality Guarantee

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Compound Identifiers

PubChem CID

101886309 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	1612191-86-2
MW:	392.6
Formula:	C₂₅H₄₄O₃

BAR502

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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