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GB83 

Cat. No. M28045
GB83  Structure
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Biological Activity

GB83 is a potent PAR2 antagonist. GB83 reverses neutrophil elastase‐induced synovitis and pain. GB83 blocks the effect of MET-1 supernatant on NG neurons.

Chemical Information
Molecular Weight 548.72
Formula C32H44N4O4
CAS Number 1252806-86-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yunkyung Heo, et al. Int J Mol Sci. GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP

[2] EunJin Bang, et al. Redox Biol. Protease-activated receptor 2 induces ROS-mediated inflammation through Akt-mediated NF-κB and FoxO6 modulation during skin photoaging

[3] Yohan Seo, et al. Br J Pharmacol. Novel positive allosteric modulator of protease-activated receptor 1 promotes skin wound healing in hairless mice

[4] Ji Yun Her, et al. Am J Physiol Gastrointest Liver Physiol. Blockage of protease-activated receptor 2 exacerbates inflammation in high-fat environment partly through autophagy inhibition

[5] Flora Lucena, et al. Neurosci Lett. Pain responses to protease-activated receptor-2 stimulation in the spinal cord of naïve and arthritic rats

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  Catalog
Abmole Inhibitor Catalog




Keywords: GB83  supplier, PAR, inhibitors, activators


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