MS47134 is a potent and specific MRGPRX4 agonist/activator with EC50 of 149 nM. MS47134 may be utilized to study pain, itch, and mast cell-mediated hypersensitivity.

Physicochemical Properties

Molecular Formula	C22H29NO3
Molecular Weight	355.47
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
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	EC50: 149 nM (MRGPRX4)[1]
ln Vitro	In the FLIPR Ca2+ test, MS47134 is more potent than nateglinide as an MRGPRX4 agonist [1]. The Kir6.2/SUR1 potassium channel exhibits 47-fold enhanced selectivity for MRGPRX4 when using MS47134 (0.001 nM-0.1 mM)[1]. Relatively recently, a family of mas-related G-protein-coupled receptors known as the MRGPRX family of receptors (MRGPRX1-4) developed. Important physiological and pathological mediators of itching and associated mast cell-mediated hypersensitivity reactions include MRGPRX2 and MRGPRX4[1].
References	[1]. Structure, function and pharmacology of human itch GPCRs. Nature. 2021 Dec;600(7887):170-175.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~281.32 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.03 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 25.0 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: ≥ 2.5 mg/mL (7.03 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (7.03 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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	2.8132 mL	14.0659 mL	28.1318 mL
	5 mM	0.5626 mL	2.8132 mL	5.6264 mL
	10 mM	0.2813 mL	1.4066 mL	2.8132 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.