2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. 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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Based on 1 publication(s) in Google Scholar

GB83 Related Antibodies

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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.

GB83 Related Antibodies
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 : 50 mg/mL (91.12 mM; Need ultrasonic; 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

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% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.56 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO 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% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.56 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 DMSO 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)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.80%

SDS (251 KB)

COA (255 KB)

Handling Instructions (2659 KB)
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
80 mM 0.0228 mL 0.1139 mL 0.2278 mL 0.5695 mL
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GB83 Related Classifications

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:

GB831252806-86-2GB 83GB-83Protease Activated Receptor (PAR)Thrombin receptorsneutrophil elastasesynovitispainPAR2 KO miceNG neuronsInhibitorinhibitorinhibit

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