1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. Desmethylazelastine

Desmethylazelastine 是 Azelastine 通过细胞色素 P450 酶系统氧化代谢的主要活性代谢物,其蛋白结合率为 97%,消除半衰期为 54 小时。Azelastine 是一种具有口服活性、选择性和高亲和力的组胺 H1 受体拮抗剂。Azelastine 可用于过敏性鼻炎、哮喘、糖尿病高脂血症以及 SARS-CoV-2 的研究。

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Desmethylazelastine Chemical Structure

Desmethylazelastine Chemical Structure

CAS No. : 47491-38-3

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Other Forms of Desmethylazelastine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4][5].

体内研究
(In Vivo)

1.19 Pharmacokinetic parameters of desmethylazelastine after a single oral administration of 1.0 mg/kg azelastine hydrochloride in guinea pigs[1].

Blood Lung
Cmax (ng/mL)[a] 17.6 2863
Tmax (h) 3.0-6.0 4.0-6.0
Tlag (h) 0.25 0.39
AUC0-24 (ng•h/mL)[a] 180 28502
t1/2 (h) 4.24 3.90
CL (L/h) 0.213
Lung-blood ratio[b] 146 146
[a] For lung, the unit in grams (g) instead of milliliter (mL). [b] Mean value calculated from all time points.

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

分子量

367.87

Formula

C21H22ClN3O

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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  • 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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产品名称:
Desmethylazelastine
目录号:
HY-147336
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