Asapiprant

SKU: orb1301834

Description

Asapiprant (S-555739) is a highly selective DP1 receptor antagonist with sub-nanomolar potency (Ki = 0.44 nM). This tool compound is used in research to investigate the role of the DP1 receptor in allergic inflammation and asthma, supporting both in vitro binding studies and in vivo disease models.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 932372-01-5
• MW: 501.55
• Purity: 99.64%
• Formula: C₂₄H₂₇N₃O₇S
• SMILES: CC(C)Oc1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(-c2ncco2)c(OCC(O)=O)c1
• Target: Prostaglandin Receptor
• Solubility: DMSO:10 mg/mL (19.94 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.99 mM)

Bioactivity

• Target IC50:
  DP1 receptor:0.44 nM (Ki)
• 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.
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DP1, Asapiprant, Inhibitor, inhibit, S555739, S-555739, S 555739, ProstaglandinReceptor, Prostaglandin Receptor

Compound Identifiers

PubChem CID

59232326