1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. GB-88

GB-88 

Cat. No.: HY-120261
Handling Instructions

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

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

GB-88 Chemical Structure

GB-88 Chemical Structure

CAS No. : 1416435-96-5

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Description

GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 µM[1].

IC50 & Target

PAR2[1]

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[1].

In Vivo

GB-88 (10 mg/kg, p.o. in olive oil) 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)[1].
GB-88 inhibits PAR2-induced acute inflammation in vivo[1].

Animal Model: Male Wistar rats (8–9 weeks)[1]
Dosage: 10 mg/kg
Administration: Oral gavage in olive oil
Result: Was 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).
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

546.70

Formula

C₃₂H₄₂N₄O₄

CAS No.

1416435-96-5

SMILES

O=C([[email protected]]([[email protected]@H](C)CC)NC([[email protected]](CC1CCCCC1)NC(C2=CC=NO2)=O)=O)N3CCC4(C=CC5=C4C=CC=C5)CC3

Shipping

Room temperature in continental US; may vary elsewhere

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GB-88
Cat. No.:
HY-120261
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GB-88

Cat. No.: HY-120261