| Name | Asapiprant |
| Description | 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. |
| Cell Research | 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. |
| Animal Research | 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. |
| In vitro | 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. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 10 mg/mL (19.94 mM)
|
| Keywords | S-555739 | S555739 | S 555739 | Prostaglandin Receptor | Inhibitor | inhibit | Asapiprant |
| Inhibitors Related | Angoroside C | Pranoprofen | Tranilast | Benorilate | Rutin | Ozagrel | Ethamsylate | Rebamipide | Tebufelone | Evodiamine | Timapiprant | p-Hydroxycinnamic acid |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
