| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
MrgprX2 antagonist-8 selectively targets MrgprX2 (Mas-related G-protein coupled receptor X2), a receptor expressed on mast cells. Activation of MrgprX2 by various ligands triggers mast cell degranulation and pseudo-allergic reactions. Antagonism of this receptor is a therapeutic strategy for inflammatory and allergic diseases.
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| ln Vitro |
MrgprX2 antagonist-8 demonstrates antagonist activity against MrgprX2 with IC50 values of 100-500 nM in LAD2 mast cell hexosaminidase release assays and <100 nM in CHO cell-based functional assays. It effectively inhibits MrgprX2 signaling, making it useful for investigating the receptor's role in inflammation.
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| ln Vivo |
Dedicated in vivo efficacy studies for MrgprX2 antagonist-8 are not extensively documented in standard profiles. As a tool for researching inflammatory disorders, it is hypothesized to reduce mast cell-driven inflammation in animal models, but detailed in vivo data are not publicly available.
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| Enzyme Assay |
The antagonist activity is measured using a cell-based functional assay rather than a cell-free enzyme assay. CHO cells expressing recombinant MrgprX2 are incubated with a known MrgprX2 agonist and varying concentrations of MrgprX2 antagonist-8. Receptor activation is measured using a calcium flux assay or a reporter gene readout.
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| Cell Assay |
LAD2 human mast cells are cultured and treated with MrgprX2 antagonist-8. Cells are then stimulated with a known MrgprX2 agonist (e.g., substance P or compound 48/80). Mast cell degranulation is measured by quantifying the release of hexosaminidase or beta-hexosaminidase into the culture supernatant.
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| Animal Protocol |
Dedicated in vivo protocols for MrgprX2 antagonist-8 are not well-documented. A standard protocol would involve a murine model of passive cutaneous anaphylaxis or a model of mast cell-dependent inflammation. The compound would be administered prior to challenge with an MrgprX2 agonist.
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| ADME/Pharmacokinetics |
Detailed PK parameters for MrgprX2 antagonist-8 are not extensively documented. The compound has high solubility in DMSO (>100 mg/mL), which facilitates formulation for both in vitro and in vivo studies. Comprehensive ADME data are not publicly reported.
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| Toxicity/Toxicokinetics |
Toxicological data for MrgprX2 antagonist-8 are not available in standard profiles. As a research chemical, comprehensive toxicology studies have not been performed. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
MrgprX2 antagonist-8 is a valuable pharmacological tool for investigating mast cell biology and the mechanisms underlying allergic and inflammatory diseases. It holds therapeutic potential for conditions like chronic urticaria and drug-induced hypersensitivity. It is not an approved drug.
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| Molecular Formula |
C24H24CLF3N4O3S
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|---|---|
| Molecular Weight |
540.99
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| Exact Mass |
540.12
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| CAS # |
2768216-96-0
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| PubChem CID |
163267276
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| Appearance |
White to off-white solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
864
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N[C@@H]1CC[C@H](NC2C3C(N=C(C(F)(F)F)C=2)=CC=C(Cl)C=3)CC1)(=O)C1=CC=CC(NS(C)(=O)=O)=C1
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| InChi Key |
OYVIDGWBLJUXIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24ClF3N4O3S/c1-36(34,35)32-18-4-2-3-14(11-18)23(33)30-17-8-6-16(7-9-17)29-21-13-22(24(26,27)28)31-20-10-5-15(25)12-19(20)21/h2-5,10-13,16-17,32H,6-9H2,1H3,(H,29,31)(H,30,33)
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| Chemical Name |
N-[4-[[6-chloro-2-(trifluoromethyl)quinolin-4-yl]amino]cyclohexyl]-3-(methanesulfonamido)benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 250 mg/mL (~462.12 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (20.8 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.08 mg/mL (3.84 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 DMSO stock solution (20.8 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8485 mL | 9.2423 mL | 18.4846 mL | |
| 5 mM | 0.3697 mL | 1.8485 mL | 3.6969 mL | |
| 10 mM | 0.1848 mL | 0.9242 mL | 1.8485 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.
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