1. GPCR/G Protein
  2. Protease Activated Receptor (PAR)
  3. GB83

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.

For research use only. We do not sell to patients.

GB83 Chemical Structure

GB83 Chemical Structure

CAS No. : 1252806-86-2

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Description

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[1].

IC50 & Target[1]

PAR2

 

In Vitro

GB83 (10 μM) blocks the effect of MET-1 (microbial ecosystem therapeutic-1) supernatant on nodose ganglion (NG) neurons[2].

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

In Vivo

GB83 (5 μg; i.p.) reverses neutrophil elastase‐induced synovitis and pain in PAR2 KO mice[1].

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

Animal Model: 8-14 weeks, 20-30 g male C57Bl/6 mice (PAR2 KO mice)[1]
Dosage: 5 µg
Administration: I.p.; 3 times at 10 min before and 110 and 230 min after neutrophil elastase administered
Result: Significantly blocked the neutrophil elastase induced increase in vascular perfusion, as well as the number of rolling adherent leukocytes, and also significantly attenuated hindpaw allodynia.
Molecular Weight

548.72

Formula

C32H44N4O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=NO1)N[C@@H](CC2CCCCC2)C(N[C@@H]([C@@H](C)CC)C(N3CCC4(CC3)C5=CC=CC=C5CC4)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (72.90 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8224 mL 9.1121 mL 18.2242 mL
5 mM 0.3645 mL 1.8224 mL 3.6448 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.8%

References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8224 mL 9.1121 mL 18.2242 mL 45.5606 mL
5 mM 0.3645 mL 1.8224 mL 3.6448 mL 9.1121 mL
10 mM 0.1822 mL 0.9112 mL 1.8224 mL 4.5561 mL
15 mM 0.1215 mL 0.6075 mL 1.2149 mL 3.0374 mL
20 mM 0.0911 mL 0.4556 mL 0.9112 mL 2.2780 mL
25 mM 0.0729 mL 0.3645 mL 0.7290 mL 1.8224 mL
30 mM 0.0607 mL 0.3037 mL 0.6075 mL 1.5187 mL
40 mM 0.0456 mL 0.2278 mL 0.4556 mL 1.1390 mL
50 mM 0.0364 mL 0.1822 mL 0.3645 mL 0.9112 mL
60 mM 0.0304 mL 0.1519 mL 0.3037 mL 0.7593 mL
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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.

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Product Name:
GB83
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HY-124061
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