2. GPCR/G Protein Apoptosis
  3. Mas-related G-protein-coupled Receptor (MRGPR) TNF Receptor
  4. Z-3578

Z-3578 是一种靶向 MrgX2 (Mas-related G protein-coupled receptor X2) 的小分子拮抗剂，具有显著的抗假性过敏活性，KD 值为 729 nM。Z-3578 能有效抑制 substance P (SP) 和 C48/80 诱导的肥大细胞脱颗粒，抑制 β-hexosaminidase 的释放，IC50 分别为 4.90 µM 和 6.18 µM，并显著降低组胺和 TNF-α 的释放，减少细胞内钙流。此外，Z-3578 在小鼠假性过敏模型中可显著减轻足部肿胀和染料渗出，降低血清组胺水平，提示其体内亦具备良好的抗过敏效应。Z-3578 有望作为抗过敏领域特别是假性过敏反应的候选先导化合物。

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Z-3578 Chemical Structure

Z-3578 Chemical Structure

CAS No. : 473687-20-6

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Z-3578 相关抗体

Top Publications Citing Use of Products

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions[1].

分子量

467.37

Formula

C23H16Cl2N4OS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Z-3578 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Z-3578473687-20-6Z3578Z 3578Mas-related G-protein-coupled Receptor (MRGPR)TNF ReceptorTumor Necrosis Factor ReceptorTNFRInhibitorinhibitorinhibit

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目录号：
HY-172458
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