BAR502

Name: BAR502
Brand: MedChemExpress
SKU: HY-101273
Rating: 4.5 (1 reviews)

Cat. No.: HY-101273 Purity: 99.53%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1612191-86-2

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in Ethanol	USD 187	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1380	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
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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]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.4 μM Compound: 30, NorECDCOH	Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay Agonist activity at GP-BAR1 (unknown origin) in human HEK293 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by CRE-driven luciferase reporter gene assay	[PMID: 25247751]
HepG2	EC₅₀	2 μM Compound: 30, NorECDCOH	Agonist activity at FXR (unknown origin) expressed in human HepG2 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by FXR response element driven HSP27-TK-luciferase reporter gene assay Agonist activity at FXR (unknown origin) expressed in human HepG2 cells assessed as receptor transactivation at 100 nM to 50 uM incubated for 16 hrs by FXR response element driven HSP27-TK-luciferase reporter gene assay	[PMID: 25247751]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

392.62

Formula

C₂₅H₄₄O₃

CAS No.

1612191-86-2

Appearance

Solid

Color

White to off-white

SMILES

C[C@H](CCO)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMF : 50 mg/mL (127.35 mM; Need ultrasonic)

Ethanol : ≥ 50 mg/mL (127.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.53%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (250 KB) RP-HPLC (209 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Animal Administration
^[2]

Mice: 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

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMF / Ethanol	1 mM	2.5470 mL	12.7350 mL	25.4699 mL	63.6748 mL
	5 mM	0.5094 mL	2.5470 mL	5.0940 mL	12.7350 mL
	10 mM	0.2547 mL	1.2735 mL	2.5470 mL	6.3675 mL
	15 mM	0.1698 mL	0.8490 mL	1.6980 mL	4.2450 mL
	20 mM	0.1273 mL	0.6367 mL	1.2735 mL	3.1837 mL
	25 mM	0.1019 mL	0.5094 mL	1.0188 mL	2.5470 mL
	30 mM	0.0849 mL	0.4245 mL	0.8490 mL	2.1225 mL
	40 mM	0.0637 mL	0.3184 mL	0.6367 mL	1.5919 mL
	50 mM	0.0509 mL	0.2547 mL	0.5094 mL	1.2735 mL
	60 mM	0.0424 mL	0.2122 mL	0.4245 mL	1.0612 mL
	80 mM	0.0318 mL	0.1592 mL	0.3184 mL	0.7959 mL
	100 mM	0.0255 mL	0.1273 mL	0.2547 mL	0.6367 mL

BAR502 Related Classifications

Neurological Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAR5021612191-86-2BAR 502BAR-502G protein-coupled Bile Acid Receptor 1FXRAutophagyG-protein coupled receptor 19GPCR19TGR5GPBAR1NR1H4Inhibitorinhibitorinhibit

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BAR502

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Complete Stock Solution Preparation Table

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