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GB-88

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Catalog No. T11370Cas No. 1416435-96-5

GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.

GB-88

GB-88

😃Good
Catalog No. T11370Cas No. 1416435-96-5
GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
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5 mg423 €7-10 days
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Product Introduction

Bioactivity
Description
GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
In vitro
GB-88 inhibits iCa2+ release induced in HT29 cells by trypsin, 2f-LIGRLO-NH2 and GB110 (PAR2 agonists).?And antagonism by GB-88 is agonist dependent.
In vivo
GB-88 inhibits PAR2-induced acute inflammation in vivo.GB-88 is both orally active and anti-inflammatory in vivo, with specific antagonist activity against four structurally and mechanistically different PAR2 agonists (2f-LIGRLO-NH2, trypsin, SLIGRL-NH2 and GB110).
Chemical Properties
Molecular Weight546.7
FormulaC32H42N4O4
Cas No.1416435-96-5
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 31.25 mg/mL (57.16 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8292 mL9.1458 mL18.2916 mL91.4578 mL
5 mM0.3658 mL1.8292 mL3.6583 mL18.2916 mL
10 mM0.1829 mL0.9146 mL1.8292 mL9.1458 mL
20 mM0.0915 mL0.4573 mL0.9146 mL4.5729 mL
50 mM0.0366 mL0.1829 mL0.3658 mL1.8292 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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