| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
EC50: 149 nM (MRGPRX4)[1]
MS47134 targets the Mas-related G protein-coupled receptor X4 (MRGPRX4), a GPCR expressed in sensory neurons and mast cells. It acts as a potent and selective agonist, activating Gq-mediated signaling pathways. MRGPRX4 is involved in the transmission of itch signals and mast cell activation, making it a therapeutic target for pruritic conditions. |
|---|---|
| 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].
MS47134 is a potent and selective MRGPRX4 agonist with an EC50 value of 149 nM. It activates MRGPRX4 with high selectivity over other MRGPR family members, enabling specific studies of MRGPRX4-mediated signaling pathways in sensory neurons and immune cells. |
| Enzyme Assay |
A standard in vitro MRGPRX4 agonist assay involves using HEK293 cells stably or transiently expressing human MRGPRX4 and a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM). Cells are loaded with the dye in HBSS buffer for 30-60 minutes at 37degC. Varying concentrations of MS47134 (0.1-10,000 nM) are added to the cells, and intracellular calcium flux (increase in fluorescence, excitation 488 nm, emission 525 nm) is measured in real-time using a fluorescence plate reader. The EC50 (149 nM) is calculated by fitting a four-parameter logistic curve.
|
| Animal Protocol |
Not available. For in vivo studies, standard protocols involve administering MS47134 to mice (e.g., by intradermal or intrathecal injection) to induce itch-related scratching behavior. The number of scratching bouts is recorded over a defined period (e.g., 30-60 minutes). Histological analysis of skin or spinal cord tissues can be performed to assess mast cell degranulation, neuroinflammation, or neuronal activation markers such as c-Fos.
|
| ADME/Pharmacokinetics |
MS47134 is a small molecule with an EC50 of 149 nM for MRGPRX4. For in vitro use, it is soluble in DMSO to prepare stock solutions. For in vivo formulation, it can be dissolved in saline containing 5-10% DMSO, 5% Tween-80, or other co-solvents. Its physicochemical properties (molecular weight, logP) are not detailed in the literature.
|
| Toxicity/Toxicokinetics |
No specific toxicological data for MS47134 is available. As an MRGPRX4 agonist, its toxicity would be related to its mechanism of action: activation of MRGPRX4 can induce itching, pain, and mast cell degranulation, which may cause localized inflammation and discomfort at the site of injection. Chronic activation could potentially lead to neuropathic changes or persistent hypersensitivity.
|
| References | |
| Additional Infomation |
MS47134 is a research-grade selective MRGPRX4 agonist. Its non-deuterated parent (MS47134) has been used in cryo-EM structural studies to elucidate the MRGPRX4 activation mechanism (PDB structure 7s8p). It is not a drug and has not been approved for any therapeutic indication. This product is strictly for laboratory research in the fields of pain, itch biology, mast cell biology, and GPCR signaling.
|
| 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)
|
| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
