Asapiprant

Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1, Ki = 0.44 nM). It is selective for DP1 over DP2, as well as the thromboxane A2 (TXA2), prostaglandin I2 (PGI2), and prostaglandin E1-4 (PGE1-4) receptors (Kis = >5,000, >4,800, >6,300, and 120->6,600 nM, respectively). Asapiprant (1 and 3 mg/kg) reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis. It reduces nasal secretion, when administered at doses of 3 and 30 mg/kg, and antigen-induced cell infiltration in nasal lavage fluids, when administered at 3 and 10 mg/kg, in a guinea pig model of allergic rhinitis induced by ovalbumin. Asapiprant (10 mg/kg) also decreases airway hyperresponsiveness, inflammatory cell infiltration in bronchoalveolar lavage fluid (BALF), and mucin production in a rat model of ovalbumin-induced asthma.Formal Name: 2-[5-[4-[[4-(1-methylethoxy)phenyl]sulfonyl]-1-piperazinyl]-2-(2-oxazolyl)phenoxy]-acetic acid. CAS Number: 932372-01-5. Synonyms: S-555739. Molecular Formula: C24H27N3O7S. Formula Weight: 501.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml, DMSO: 3 mg/ml. lambdamax: 242, 318 nm. SMILES: OC(COC1=CC(N2CCN(S(C3=CC=C(OC(C)C)C=C3)(=O)=O)CC2)=CC=C1C4=NC=CO4)=O. InChi Code: InChI=1S/C24H27N3O7S/c1-17(2)34-19-4-6-20(7-5-19)35(30,31)27-12-10-26(11-13-27)18-3-8-21(24-25-9-14-32-24)22(15-18)33-16-23(28)29/h3-9,14-15,17H,10-13,16H2,1-2H3,(H,28,29). InChi Key: ZMZNWNTZRWXTJU-UHFFFAOYSA-N.