1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. AY 25674

AY 25674 是一种口服有效的抗过敏剂与 PDE 抑制剂。AY 25674 可抑制肥大细胞中过敏性组胺的释放。AY 25674 可抑制由反应素型 (IgE) 抗体诱导的被动过敏反应。AY 25674 不会抑制由非反应素型抗体、血清素或组胺引起的血管通透性增加。AY 25674 在给药后不久即达活性峰值;大剂量使用会产生快速耐受现象。AY 25674 可用于被动过敏反应的相关研究。

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AY 25674

AY 25674 Chemical Structure

CAS No. : 65425-48-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AY 25674 is an orally active antiallergic agent and a PDE inhibitor. AY 25674 inhibits the release of allergic histamine from mast cells. AY 25674 suppresses passive anaphylaxis induced by reaginic (IgE) antibodies. AY 25674 does not inhibit the increased vascular permeability caused by non-reaginic antibodies, serotonin or histamine. AY 25674 reaches its peak activity shortly after administration; rapid tolerance occurs at high doses. AY 25674 can be used in research related to passive anaphylaxis[1][2].

体外研究
(In Vitro)

AY-25,674 在牛心脏环 3',5'- PDE 活性抑制体外实验中,对牛心脏 PDE 的酶活性产生显著抑制作用,其抑制效力约为茶碱的 1/3[1]
AY-25,674 (1×10-4 M;15 min) 在豚鼠肺腺苷酸环化酶活性检测体外实验中,仅使无 PDE 活性的豚鼠肺腺苷酸环化酶基础活性提升 7%,无显著的直接激活环腺苷酸 (cAMP) 生成的作用[1]

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

体内研究
(In Vivo)

AY 25674 (1-100 mg/kg;静脉注射、腹腔注射、口服) 可剂量依赖性地抑制大鼠中由反应素介导的被动足爪过敏水肿,口服给药后 5 分钟时活性达峰值,大剂量重复给药会诱导快速耐受,其相对效力与其他口服抗过敏药物相当[2]
AY 25674 (10 mg/kg;静脉注射) 可特异性抑制大鼠体内由反应素介导的毛细血管通透性升高,而对非反应素机制或介质直接作用诱导的通透性改变无显著影响[2]
AY 25674 (0.01-0.3 mg/kg 腹腔注射;30-300 mg/kg 口服) 可剂量依赖性地抑制大鼠腹膜肥大细胞中由反应素介导的组胺释放,且口服给药的效力较低[2]

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

Animal Model: Charles River rats (180-200 g)[2]
Dosage: 0.01-0.3 mg/kg (i.p.); 30-300 mg/kg (oral)
Administration: i.p. (15-30 seconds before antigen challenge); oral (5 minutes before antigen challenge)
Result: Inhibited histamine release from sensitized peritoneal mast cells in a dose-dependent manner via both intraperitoneal and oral routes.
Required approximately 100 times more oral dose to achieve comparable inhibition to intraperitoneal administration.
Nonspecific histamine release was 2.2%.
分子量

221.21

Formula

C11H11NO4

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
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    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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产品名称:
AY 25674
目录号:
HY-165395
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