化合物Asapiprant T5386

Product Introduction
Bioactivity


英文名: Asapiprant

描述: 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。

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (19.94 mM)


关键字: S 555739 | Prostaglandin Receptor | inhibit | Asapiprant | S555739 | Inhibitor | S-555739

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相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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