Asapiprant 是一个强效且有选择性的 DP₁ 受体拮抗剂，其 K_i 值为 0.44 nM。

Asapiprant is a potent and selective DP 1 receptor antagonist with a K i of 0.44 nM.

Solid

Ki: 0.44 nM (DP1 receptor)

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) D 2 (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 signi

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 11.11 mg/mL (22.15 mM; Need ultrasonic)配制储备液