Asapiprant

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Chemical Structure| 932372-01-5 同义名 : S-555739
CAS号 : 932372-01-5
货号 : A724929
分子式 : C24H27N3O7S
纯度 : 99%+
分子量 : 501.55
MDL号 : MFCD28902252
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.94mL

3.99mL

1.99mL

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