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GB-88

Name: GB-88
Brand: TargetMol
SKU: T11370
Rating: 4.5 (1 reviews)

(Synonyms: GB88, GB 88) Copy Product Info

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Synonyms: GB88, GB 88

Catalog No. T11370 Copy Product Info

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GB-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-NH₂, 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.

Cas No. 1416435-96-5

Pack Size	Price	USA Stock	Global Stock	Quantity
5 mg	$446	7-10 days	7-10 days

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	GB-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-NH₂, 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.
Targets & IC50	PAR2:2 μM
In vitro	Methods: 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 vivo	Methods: 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]
Synonyms	GB88, GB 88

Chemical Properties

Molecular Weight	546.70
Formula	C₃₂H₄₂N₄O₄
Cas No.	1416435-96-5
Smiles	C([C@@H](NC([C@H](CC1CCCCC1)NC(=O)C2=CC=NO2)=O)[C@H](CC)C)(=O)N3CCC4(C=5C(C=C4)=CC=CC5)CC3
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25.00 mg/mL (45.73 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.00 mg/mL (3.66 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8292 mL	9.1458 mL	18.2916 mL	91.4578 mL
5 mM	0.3658 mL	1.8292 mL	3.6583 mL	18.2916 mL
10 mM	0.1829 mL	0.9146 mL	1.8292 mL	9.1458 mL
20 mM	0.0915 mL	0.4573 mL	0.9146 mL	4.5729 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.