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CAS No.: 932372-01-5

Asapiprant Catalog No. CSN25356

Synonyms: S-555739

Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM. Significant suppression of antigen-induced nasal resistance, nasal secretion, and cell infiltration in nasal mucosa was observed with asapiprant treatment. In addition, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly suppresses the increase in nasal resistance by 82% and 92%, respectively. Asapiprant at 5 mg/kg suppresses Prostaglandin PGD2-induced nasal resistance by 86%. When orally administered 1 h before the antigen challenge in pigs, Asapiprant (3, 10, and 30 mg/kg) suppresses immediate airway response (IAR) by 52%, 57%, and 96%, and late airway response (LAR) by 67%, 50%, and 79%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly reduces airway hyper-responsiveness (AHR), infiltration of inflammatory cells, and mucin production in bronchoalveolar lavage fluid (BALF), although treatment with Asapiprant at 0.1 mg/kg does not have a significant effect on any responses^[1].
参考文献

[1] Takahashi G, Asanuma F, Suzuki N, et al. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur J Pharmacol. 2015;765:15‐23

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9938 mL
- 9.9691 mL
- 19.9381 mL
- 5 mM
- 0.3988 mL
- 1.9938 mL
- 3.9876 mL
- 10 mM
- 0.1994 mL
- 0.9969 mL
- 1.9938 mL

技术信息

CAS号

932372-01-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H27N3O7S

运输

蓝冰

分子量

501.55

别名

S-555739

溶解度

DMSO	11.0 mg/mL (21.9 mM) warming

动物实验配方

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