1. GPCR/G Protein
    Metabolic Enzyme/Protease
  2. GPCR19
    FXR

BAR502 

Cat. No.: HY-101273 Purity: >98.0%
Data Sheet SDS Handling Instructions

BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.

For research use only. We do not sell to patients.
BAR502 Chemical Structure

BAR502 Chemical Structure

CAS No. : 1612191-86-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO $285 In-stock
1 mg $110 In-stock
5 mg $330 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.

IC50 & Target

IC50: 2 μM (FXR), 0.4 μM (GPBAR1)[1]

In Vitro

BAR502 is a truncated side chain alcohol with both substituents on ring B in α-configuration. 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 pro-glucagon 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 a very potent activity in the recruitment of SRC-1 coactivator and high affinity to FXR[1].

In Vivo

Treatment with BAR502 causes a 10% reduction of b.w., increases insulin sensitivity and circulating levels of HDL, while reduces steatosis, inflammatory and fibrosis scores and liver expression of SREPB1c, FAS, PPARγ, CD36 and CYP7A1 mRNA. BAR502 increases the expression of SHP and ABCG5 in the liver and SHP, FGF15 and GLP1 in intestine. BAR502 promotes the browning of epWAT and reduces liver fibrosis induced by CCl4[2]. In models of non-obstructive cholestasis, BAR502 attenuates liver injury without causing itching. Co-treatment with BAR502 increases survival, attenuates serum alkaline phosphatase levels and robustly modulates the liver expression of canonical FXR target genes including OSTα, BSEP, SHP and MDR1, without inducing pruritus[3].

References
Animal Administration
[2]

BAR502 is prepared in 1% methyl cellulose in drinking water.

Mouse: 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[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

392.62

Formula

C₂₅H₄₄O₃

CAS No.

1612191-86-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
BAR502
Cat. No.:
HY-101273
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