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GB-88

Catalog No. T11370   CAS 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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GB-88 Chemical Structure
GB-88, CAS 1416435-96-5
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Molecular Weight 546.7
Formula C32H42N4O4
CAS No. 1416435-96-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31.25 mg/mL (57.16 mM), sonification is recommended.

TargetMolReferences and Literature

1. Suen JY, et al. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GB-88 1416435-96-5 Others GB 88 GB88 inhibitor inhibit

 

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