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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.72%
- CAS 番号: 473687-20-6
- 分子式: C23H16Cl2N4OS
- 分子量:467.37
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保管条件:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Z-3578
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生物活性
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.
化学情報
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CAS 番号 473687-20-6
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性状 Solid
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分子量 467.37
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-172458 関連分類
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