Z-3578
Based on 1 publication(s) in Google Scholar
Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions.
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- Pureza: 98.72%
- No. CAS: 473687-20-6
- Fòrmula: C23H16Cl2N4OS
- Peso molecular:467.37
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Z-3578
MoreVer todos los productos específicos de isoformas TNF Receptor
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Actividad biológica
Z-3578 potently inhibits β-hexosaminidase release from human mast cell line LAD2 induced by SP (HY-P0201) and C48/80 (HY-130592), with IC50 values of 4.90 μM and 6.18 μM[1].
Z-3578 (1-10 μM) concentration-dependently inhibits SP-induced histamine release from LAD2 human mast cells[1].
Z-3578 (1-10 μM; 6 h) concentration-dependently inhibits SP-induced TNF-α release from human mast cell line LAD2[1].
Z-3578 (10 μM; 30 min) inhibits intracellular calcium mobilization in MrgX2-His-tag-HEK293 cells and blocks MrgX2-mediated signaling pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LAD2 human mast cell
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Concentration:1, 5 and 10 μM
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Incubation Time:6 h
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Result:Reduced SP-induced TNF-α release in a concentration-dependent manner.
Showed significant inhibition at all tested concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks old)[1]
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Dosage:0.1 mg/mL; 0.5 mg/mL; 1 mg/mL; 1 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.g.; single dose
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Result:Significantly reduced paw edema induced by C48/80 in mice at concentrations of 0.5 and 1.0 mg/mL.
Significantly decreased Evans blue extravasation at a concentration of 1.0 mg/mL.
Markedly lowered serum histamine release induced by C48/80.
Attenuated mast cell degranulation in the mouse paw skin induced by C48/80.
Chemical Information
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No. CAS 473687-20-6
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Appearance Solid
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Peso molecular 467.37
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Fòrmula C23H16Cl2N4OS
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Color White to light yellow
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SMILES
O=C(CSC1=NC(C2=CC=CC=C2)=C(N=N1)C3=CC=CC=C3)NC4=C(C=C(C=C4)Cl)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cells
Identification of Natural Compounds Triggering MRGPRX2-Mediated Calcium Flux and Degranulation in RBL-2H3 Cells. [Abstract]2026 Feb 3;15(3):287. PMID: 41677650
Solvente y solubilidad
DMSO : 25 mg/mL (53.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1396 mL | 10.6982 mL | 21.3963 mL | 53.4908 mL |
| 5 mM | 0.4279 mL | 2.1396 mL | 4.2793 mL | 10.6982 mL | |
| 10 mM | 0.2140 mL | 1.0698 mL | 2.1396 mL | 5.3491 mL | |
| 15 mM | 0.1426 mL | 0.7132 mL | 1.4264 mL | 3.5661 mL | |
| 20 mM | 0.1070 mL | 0.5349 mL | 1.0698 mL | 2.6745 mL | |
| 25 mM | 0.0856 mL | 0.4279 mL | 0.8559 mL | 2.1396 mL | |
| 30 mM | 0.0713 mL | 0.3566 mL | 0.7132 mL | 1.7830 mL | |
| 40 mM | 0.0535 mL | 0.2675 mL | 0.5349 mL | 1.3373 mL | |
| 50 mM | 0.0428 mL | 0.2140 mL | 0.4279 mL | 1.0698 mL |
Z-3578 Related Classifications
HY-172458 Related Classifications
Powered by Bioz
- Z-3578
- 473687-20-6
- Z3578
- Z 3578
- Mas-related G-protein-coupled Receptor (MRGPR)
- TNF Receptor
- mast cell degranulation
- inflammatory mediator release
- pseudoallergy
- male C57BL/6 mice
- MrgX2-His-tag-HEK293 cells
- LAD2 human mast cells
- MrgX2
- Evans blue extravasation
- paw swelling
- calcium mobilization
- Inhibitor
- inhibitor
- inhibit