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Asapiprant
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图片
CAS NO:932372-01-5
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
Asapiprant 是一种强选择性DP1受体拮抗剂,Ki值为 0.44 nM,对DP1受体表现出高亲和力和选择性。

产品描述

Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist (Ki: 0.44 nM). It exhibited high affinity and selectivity for the DP1 receptor.

体外活性

Asapiprant strongly inhibited the cAMP elevation elicited by PGD2 in human platelets with a half-maximal inhibitory concentration (IC50) value of 16 nM. Strong inhibition by asapiprant was observed in the cAMP elevation induced by PGD2 in guinea pigs, rats, and sheep with IC50 values (nM) of 61, 74, and 15, respectively.

体内活性

Intranasal challenge with 0.5% PGD2 led to a rapid increase in nasal resistance (sRaw) from 5 min to 60 min in sensitized guinea pigs. Oral administration of asapiprant at 1 and 3 mg/kg significantly suppressed the increase in nasal resistance by 82% and 92%, respectively. By contrast, S-5751 showed partial suppression on PGD2-induced nasal resistance in guinea pigs at 30 mg/kg by 76% that was inferior to the suppression by asapiprant at 3 mg/kg.

细胞实验

The functional antagonist activity of asapiprant on the DP1 receptor was evaluated by examining PGD2-induced elevation of cyclic adenosine monophosphate (cAMP) in platelet-rich plasma derived from venous blood (humans, guinea pigs, and sheep), and in rat DP1-transfected cells stimulated with PGD2, as described elsewhere. The functional antagonist activity of asapiprant on the DP2 receptor was evaluated by examining PGD2-induced shape change of peripheral eosinophils derived from humans and guinea pigs, as reported previously.

动物实验

After the oral administration of asapiprant or S-5751 to rats, guinea pigs, dogs, and sheep at 10 mg/kg in suspension with 0.5% methylcellulose solution, the plasma concentrations of the drugs were measured by liquid chromatography/tandem mass spectrometry or high-performance liquid chromatography.

Cas No.

932372-01-5

分子式

C24H27N3O7S

分子量

501.55

储存和溶解度

DMSO:10 mg/mL (19.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years