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  3. Pizuglanstat hydrate

Pizuglanstat hydrate  (Synonyms: TAS-205)

目录号: HY-109134A
产品使用指南 技术支持

Pizuglanstat hydrate (Compound 3;TAS-205) 是一种口服活性的前列腺素 D 合酶 (prostaglandin D synthase) 抑制剂,对人造血前列腺素 D 合酶的 IC50 为 76 nM。Pizuglanstat hydrate 抑制 PGD2 的合成。Pizuglanstat hydrate 改善实验性过敏性鼻炎。Pizuglanstat hydrate 可用于肌再生性疾病,例如肌肉营养不良研究。

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Pizuglanstat hydrate

Pizuglanstat hydrate Chemical Structure

CAS No. : 1584160-52-0

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  • 生物活性

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生物活性

Pizuglanstat hydrate (Compound 3; TAS-205) is an orally active prostaglandin D synthase inhibitor with an IC50 of 76 nM for human hematopoietic prostaglandin D synthase. Pizuglanstat hydrate inhibits the synthesis of PGD2. Pizuglanstat hydrate improves experimental allergic rhinitis. Pizuglanstat hydrate can be used in the study of muscle regenerative diseases such as muscular dystrophy[1][2][3].

体外研究
(In Vitro)

Pizuglanstat hydrate (10-3000 nM) 可抑制嗜碱性细胞 (RBL-2H3 和 KU812) 中的 PGD2 合成[2]

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

体内研究
(In Vivo)

Pizuglanstat hydrate (1-60 mg/kg;口服;单剂量或每日一次,持续 15 天) 可抑制实验性过敏性鼻炎豚鼠模型中的晚期鼻塞、嗜酸性粒细胞浸润和鼻灌洗液中的 PGD2 产生[2]

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

Animal Model: Male Hartley guinea pigs (3 weeks old at purchase, 5 weeks old at challenge); Ovalbumin (HY-W250978)-sensitized allergic rhinitis model[2]
Dosage: 1, 3, 10, 30, 60 mg/kg
Administration: Oral administration; single dose 1 h before the 3rd challenge, or once daily for 15 days
Result: Dose-dependently reduced PGD2 levels in nasal lavage fluid, suppressed late-phase nasal obstruction (area under the curve of specific airway resistance from 3-7 h).
Inhibited eosinophil infiltration into the nasal cavity.
Had additive effects on eosinophil suppression and late-phase obstruction when used in combination with Montelukast (HY-13315A), and when used in combination with Fexofenadine (HY-B0801), the suppression of early and late-phase obstruction is comparable to monotherapy.
Clinical Trial
分子量

526.63

Formula

C27H38N6O5

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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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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Pizuglanstat hydrate
目录号:
HY-109134A
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