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BAR501

Cat. No. M5223

All AbMole products are for research use only, cannot be used for human consumption.

BAR501 Structure
Size Price Availability
5mg USD 130  USD130 4-7 Days
10mg USD 220  USD220 4-7 Days
50mg USD 850  USD850 4-7 Days
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Quality Control & Documentation
Biological Activity

In vitro: BAR 501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC50 of 1 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds.

In vivo: Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mice bearing GM-CSF-secreting B16 tumors
Formulation 5% DMA, 47.5% propylene glycol
Dosages 75 mg/kg b.i.d
Administration s.c.
Chemical Information
Molecular Weight 406.64
Formula C26H46O3
CAS Number 1632118-69-4
Solubility (25°C) 10mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Barbara Renga, et al. PLoS One. Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1

[2] Cipriani S, et al. PLoS One. Impaired Itching Perception in Murine Models of Cholestasis Is Supported by Dysregulation of GPBAR1 Signaling.

[3]

[4]

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Keywords: BAR501 supplier, CGRP Receptor, inhibitors, activators

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