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Postion:Product Catalog >GB-88
GB-88
  • GB-88

GB-88 NEW

Price $446
Package 5mg
Supply Ability: 10g
Update Time: 2026-07-14

Product Details

Product Name: GB-88 CAS No.: 1416435-96-5
Supply Ability: 10g Release date: 2026/07/14

Product Introduction

Bioactivity

NameGB-88
DescriptionGB-88 is an orally active, highly selective, non-peptide PAR2 antagonist that blocks downstream inflammatory and pain signaling pathways by inhibiting PAR2-mediated Ca2? release (IC50 = 2 μM). GB-88 exhibits antagonistic activity against various PAR2 agonists, including trypsin, SLIGRL-NH?, and GB110, and shows no significant cross-reactivity with PAR1, PAR3, or PAR4. GB-88 is suitable for research into diseases such as inflammation, pain, and metabolic disorders.
In vitroMethods: A549 cells were pretreated with GB-88 (50 μM). Following pretreatment, nTyr-p39 (5 μg/ml) was added, and the cells were incubated until morphological changes occurred. Immunofluorescence staining and two-photon microscopy were used to examine cell junctions. Results: nTyr-p39 disrupted the localization of ZO-1 (tight junctions) and E-cadherin (adhesion junctions); pretreatment with GB-88 attenuated this disruption. [1] Methods: Primary rat DRG neurons were pre-incubated with GB-88 (10 μM) for 30 minutes, followed by the addition of trypsin (10 nM). Activation of DRG neurons was monitored in real time for 5 minutes using Fura-2 AM calcium imaging (340/380 nm ratio). Results: Trypsin induced a rapid, transient calcium increase; GB-88 (10 μM) suppressed both the amplitude of the response and the proportion of responding neurons.[2]
In vivoMethods: To investigate the inhibitory effects of GB-88 on protease-induced inflammation and pain, male C57BL/6 mice were administered GB-88 (10 mg/kg) via oral gavage. Two hours later, cathepsin-S (2.5 μM (0.06 U/μL), 10 μL per paw) was injected subcutaneously into the plantar region of each paw. Relevant parameters were measured 1–4 hours after injection. Results: GB-88 completely inhibited cathepsin-S-induced edema and suppressed mechanical and thermal allodynia. [2]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2.00 mg/mL (3.66 mM), Sonication is recommended.
DMSO : 25.00 mg/mL (45.73 mM), Sonication is recommended.
KeywordsPAR2 | GB-88
Inhibitors RelatedTRAP-6 amide acetate | Protease-Activated Receptor-1, PAR-1 Agonist acetate | PAR-2 Activating Peptide acetate | ML-354 | PAR-4 Agonist Peptide, amide TFA | Atopaxar | Vorapaxar sulfate | Trypsin | Vorapaxar | AY 77 | tcY-NH2 TFA(327177-34-4 free base) | 2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base)

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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