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Asapiprant(S-555739)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Asapiprant(S-555739)图片
CAS NO:932372-01-5
规格:98%
分子量:501.55
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Asapiprant是一个强效且有选择性的DP1受体拮抗剂,其Ki值为0.44nM。
CAS:932372-01-5
分子式:C24H27N3O7S
分子量:501.55
纯度:98%
存储:Store at -20°C

Background:

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



Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly (P<0.01) suppresses the increase in nasal resistance by 82% and 92%, respectively. Oral administration of Asapiprant to sheep at 5 mg/kg suppresses Prostaglandin (PG) D2 (PGD)2-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. Orally administered with Asapiprant (5 mg/kg) for 4 days, the Asapiprant significantly (P<0.01) suppresses antigen-induced nasal resistance by 73% in sheep. Treatment with 3 and 30 mg/kg of Asapiprant in pigs significantly (P<0.01) suppresses nasal secretion by 53% and 72%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly (P<0.05) 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].


[1]. Takahashi G, 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 Oct 15;765:15-23.