GB83
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.8%
- No. CAS: 1252806-86-2
- Fòrmula: C32H44N4O4
- Peso molecular:548.72
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PAR2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
2 μM
Compound: 21, GB83
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Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
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[PMID: 23895492] |
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8-14 weeks, 20-30 g male C57Bl/6 mice (PAR2 KO mice)[1]
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Dosage:5 µg
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Administration:I.p.; 3 times at 10 min before and 110 and 230 min after neutrophil elastase administered
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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.
Chemical Information
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No. CAS 1252806-86-2
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Appearance Solid
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Peso molecular 548.72
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Fòrmula C32H44N4O4
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Muley MM, et al. Neutrophil elastase induces inflammation and pain in mouse knee joints via activation of proteinase-activated receptor-2. Br J Pharmacol. 2016 Feb;173(4):766-77. [Content Brief]
[2]. Pradhananga S, et al. Protease-dependent excitation of nodose ganglion neurons by commensal gut bacteria. J Physiol. 2020 Jun;598(11):2137-2151. [Content Brief]
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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