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MRGPRX1 agonist 1

Name: MRGPRX1 agonist 1
Brand: TargetMol
SKU: T12104
Price: 90 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12104Cas No. 2377379-39-8

MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1) with an EC50 of 50 nM.

MRGPRX1 agonist 1

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Purity: 99.95%

Catalog No. T12104Cas No. 2377379-39-8

MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1) with an EC50 of 50 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$90	In Stock	In Stock
5 mg	$222	In Stock	In Stock
10 mg	$355	In Stock	In Stock
25 mg	$645	In Stock	In Stock
50 mg	$883	In Stock	In Stock
100 mg	$1,260	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$245	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.95%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

MRGPRX1 agonist 1 AI Summary

MRGPRX1 agonist 1 exhibits agonist activity at the human MrgprX1 receptor, achieving an Emax exceeding 95% and an EC50 value of 50.0 nM. It shows binding affinities with Ki values of 2470000.0 nM for the delta opioid receptor, 3730000.0 nM for the mu opioid receptor, and 12100000.0 nM for the kappa opioid receptor. The compound demonstrates a selectivity index of 50.0 for all three opioid receptors when comparing Ki values to the EC50 for its agonist activity at MrgprX1. In pharmacokinetic studies conducted in CD1 mice, MRGPRX1 agonist 1 displayed an AUC of 391.96 ng.hr.mL-1 in plasma and 5.66 nmol.hr/g in the spinal cord, with a plasma-to-spinal cord ratio of 6.3. The compound has a half-life of 0.33 hr in CD1 mice and less than 15.0 hr in mouse liver microsomes..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1) with an EC50 of 50 nM.
Targets&IC50	MRGPRX1:50 nM(EC50)

Chemical Properties

Molecular Weight	435.5
Formula	C₂₃H₂₁N₃O₄S
Cas No.	2377379-39-8
Smiles	COc1ccccc1S(=O)(=O)Nc1ccc(C)cc1Oc1ccc2c(N)nccc2c1
Relative Density.	1.365 g/cm3 (Predicted)

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: 125 mg/mL (287.03 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.18 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	2.2962 mL	11.4811 mL	22.9621 mL	114.8106 mL
5 mM	0.4592 mL	2.2962 mL	4.5924 mL	22.9621 mL
10 mM	0.2296 mL	1.1481 mL	2.2962 mL	11.4811 mL
20 mM	0.1148 mL	0.5741 mL	1.1481 mL	5.7405 mL
50 mM	0.0459 mL	0.2296 mL	0.4592 mL	2.2962 mL
100 mM	0.0230 mL	0.1148 mL	0.2296 mL	1.1481 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc