1. GPCR/G Protein Immunology/Inflammation Membrane Transporter/Ion Channel Neuronal Signaling
  2. Mas-related G-protein-coupled Receptor (MRGPR) Interleukin Related Calcium Channel
  3. BER-5

BER-5 是一种有效的 MrgX2 拮抗剂。BER-5 对多种 MrgX2 激动剂表现出广谱拮抗活性。BER-5 能够抑制 LAD2 细胞中 Substance P (SP) (HY-P0201) 诱导的脱颗粒反应,并可减轻 SP 诱导的小鼠过敏反应。BER-5 可用于过敏反应的相关机制研究。

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BER-5

BER-5 Chemical Structure

CAS No. : 724709-67-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP) (HY-P0201)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions[1].

体外研究
(In Vitro)

BER-5 (12.5-50 μM) 通过抑制 β-己糖胺酶 (30 min)、组胺 (2 h) 和 IL-8 (6 h) 的释放,特异性抑制 LAD2细胞由 SP 诱导的脱颗粒反应[1]

BER-5 (0-100 μM, 30 min) 可在 LAD2 细胞中抑制 SP 诱导的 β-己糖胺酶释放 (IC50 = 20.64 μM),效果强于 Bergaptol (BER; HY-76316) (IC50 = 46.79 μM) 和 Imperatorin (IMP; HY-N0285) (IC50 = 99.73 μM)。[1]

BER-5 (50 μM) 轻微提高了 LAD2 细胞中 SP 的半最大效应浓度 (EC50),同时显著降低了其最大效应 (Emax)[1]

BER-5 (12.5-50 μM) 能够抑制 LAD2 细胞中由 C48/80 (HY-130592)、(R)-ZINC-3573 (HY-118069)、Rocuronium Bromide (HY-17440) 和 Ciprofloxacin (HY-B0356) 药物诱导的脱颗粒反应,表明 BER-5 对多种 MrgX2 激动剂具有广谱拮抗活性[1]

BER-5 (12.5-50 μM, 30 min) 以浓度依赖的方式抑制 MrgX2-HEK293 细胞中 SP 诱导的 Ca2+ 动员[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

BER-5 (6.25-25 mg/kg, i.g., single dose) 可减轻成年小鼠中 SP 所导致的过敏反应[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks adult male C57BL/6 mice treated SP (10 μM)
Dosage: 6.25, 12.5, 25 mg/kg
Administration: i.g. 2 h before anesthetize
Result: Attenuated SP-induced local paw swelling and Evans blue exudation dose-dependently.
Mitigated SP-induced vasodilation and inhibited mast cell deformation and degranulation.
Reduced plasma histamine concentrations in a dose-dependent manner.
分子量

320.34

Formula

C20H16O4

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
  • 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.

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BER-5
目录号:
HY-174452
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