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BAR501

SKU: orb1303181

Description

BAR501 is a potent and selective agonist for the GPBAR1 receptor, exhibiting an EC50 of 1 μM. This small molecule is a valuable research tool for investigating GPBAR1's role in metabolic and inflammatory pathways, applicable in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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BAR501

Key Properties

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CAS Number1632118-69-4
MW406.64
Purity99.68% (May vary between batches)
FormulaC26H46O3
SMILESCC[C@@H]1[C@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCCO)[C@@]3(C)CC[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12
TargetGPCR19
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.92 mM);DMSO:50 mg/mL (122.96 mM)

Bioactivity

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Target IC50
GPBAR1:1 μM(EC50)
In Vivo
Pretreating rats for 6 days with BAR501 (15 mg/kg) reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. BAR501 attenuates hepatic vasomotor activity induced by methoxamine and shear stress and exerts direct vasodilatory activity in the CCl4 model. BAR501 (15 mg/kg) also reduces AST plasma levels and portal pressure, and it attenuates endothelial dysfunction by regulating CSE expression/activity.
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In Vitro
In HEK293 cells overexpressing a CRE along with GPBAR1, BAR501 effectively transactivates GPBAR1 (EC50: 1 μM). In GLUTAg cells, BAR501 (10 μM) increases the mRNA expression of GLP-1 by 2.5 folds.
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Cell Research
For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate and transfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drives the transcription of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, and with 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 μM BAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities.
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Animal Research
Animal: C57BL6 miceAdministration: i.p., 500 μL/kg of CCl4 in an equal volume of paraffin oil twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase are measured by routine biochemical clinical chemistry.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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BAR 501, BAR501, BAR-501, G-protein coupled receptor 19, G protein-coupled Bile Acid Receptor 1, GPBAR1, GPCR19, inhibit, Inhibitor, TGR5

Similar Products

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  • BAR 501 impurity

    BAR 501 impurity [orb1298661]

    99.97% (May vary between batches)

    1632118-70-7

    406.64

    C26H46O3

    5 mg, 25 mg, 1 ml x 10 mM (in DMSO), 1 mg, 10 mg
  • BAR 501 impurity

    BAR 501 impurity [orb1219471]

    >98% (HPLC)

    1632118-70-7

    406.6

    C26H46O3

    5 mg, 25 mg, 50 mg, 100 mg, 1 g, 500 mg, 200 mg, 10 mg
  • BAR 501

    BAR 501 [orb1223256]

    >98% (HPLC)

    1632118-69-4

    406.65

    C26H46O3

    10 mg, 25 mg, 100 mg, 50 mg, 1 g, 500 mg, 200 mg, 5 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
101886302 ↗

Key Properties

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No computed properties available.

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BAR501 (orb1303181)

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% DMSO +
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% Tween 80 +
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Available Sizes

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2 mg
¥ 1,040.00
5 mg
¥ 1,300.00
1 ml x 10 mM (in DMSO)
¥ 1,560.00
10 mg
¥ 1,820.00
25 mg
¥ 3,120.00
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