GB-110 HCl is a potent, orally bioactive, non-peptide protease activated receptor 2 (PAR2) agonist. GB-110 HCl selectively induces PAR2-mediated Ca2+ release in HT29 cells with EC50 of 0.28 μM.

Physicochemical Properties

Molecular Formula	C33H49CLN6O5
Molecular Weight	645.23
Related CAS #	GB-110;1252806-70-4
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	PAR2
ln Vitro	GB110 (EC50 240±20 nM; pEC50 6.7±0.05) was equivalent to the peptide agonist 2f-LIGRLO-NH2 (EC50 210±30 nM; pEC50 6.6±0.05) in an intracellular Ca2+ (iCa2+) mobilization assay using HT29 colon cancer cells. This was approximately 35 times lower than trypsin (EC50 6±0.5 nM; pEC50 8.2±0.8)[2], but 10 times stronger than SLIGRL-NH2[2].
References	[1]. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. [2]. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23.

Solubility Data

Solubility (In Vitro)

DMSO :~125 mg/mL (~193.73 mM) H2O :~25 mg/mL (~38.75 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.33 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 23.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.33 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 23.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.33 mg/mL (3.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 23.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.5498 mL	7.7492 mL	15.4983 mL
	5 mM	0.3100 mL	1.5498 mL	3.0997 mL
	10 mM	0.1550 mL	0.7749 mL	1.5498 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.