Linaprazan(Synonyms: 利那拉生; AZD0865)

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Linaprazan (Synonyms: 利那拉生; AZD0865) 纯度: 98.80%

Linaprazan (AZD0865) 能够通过K+竞争约束抑制胃里H+,K+ -ATPase. (IC 50: 1.0 ± 0.2 μM)，它对酸有很强的抑制作用。

Linaprazan(Synonyms: 利那拉生; AZD0865)

Linaprazan Chemical Structure

CAS No. : 248919-64-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1451 In-stock
5 mg ￥1800 In-stock
10 mg ￥3000 In-stock
25 mg ￥6000 In-stock
50 mg ￥9000 In-stock
100 mg ￥14000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding. (IC50: 1.0 ± 0.2 μM) It is a acid-suppressing agents with rapid onset of action and potent acid inhibition. In vitro: Linaprazan can inhibit the final step in acid secretion. Linaprazanreduced porcine renal Na+,K+-ATPase activity by 9 ± 2%, demonstrating a high selectivity for H+,K+-ATPase. In vivo: The reference for animal administration is 0.5-1.0 mg/kg. The greater degree of acid suppression with the 75-mg dose of Linaprazan would translate to a healing rate of 89% at 4 weeks.

Clinical Trial

分子量

366.46

Formula

C21H26N4O2
CAS 号

248919-64-4
中文名称

利那拉生
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 35 mg/mL (95.51 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7288 mL 13.6441 mL 27.2881 mL
5 mM 0.5458 mL 2.7288 mL 5.4576 mL
10 mM 0.2729 mL 1.3644 mL 2.7288 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Gedda K et al. Mechanism of action of AZD0865, a K+-competitive inhibitor of gastric H+,K+-ATPase. Biochem Pharmacol. 2007 Jan 15;73(2):198-205.

    [2]. Kahrilas PJ et al. A randomized, comparative study of three doses of AZD0865 and esomeprazole for healing of reflux esophagitis. Clin Gastroenterol Hepatol. 2007 Dec;5(12):1385-91.

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