Cas No.: | 932372-01-5 |
Chemical Name: | Asapiprant |
Synonyms: | Asapiprant;B2LW71CRGL;2-xy)-;A16983;BGE-175, BGE175, BGE 175 |
SMILES: | S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])(C([H])([H])[H])C([H])([H])[H])(N1C([H])([H])C([H])([H])N(C2C([H])=C([H])C(C3=NC([H])=C([H])O3)=C(C=2[H])OC([H])([H])C(=O)O[H])C([H])([H])C1([H])[H])(=O)=O |
Formula: | C24H27N3O7S |
M.Wt: | 501.5521 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | https://www.nature.com/articles/s41586-022-04630-3 |
Description: | Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.. |
In Vitro: | Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly (P<0.01) suppresses the increase in nasal resistance by 82% and 92%, respectively. Oral administration of Asapiprant to sheep at 5 mg/kg suppresses Prostaglandin (PG) D2 (PGD)2-induced nasal resistance by 86%. When orally administered 1 h before the antigen challenge in pigs, Asapiprant (3, 10, and 30 mg/kg) suppresses immediate airway response (IAR) by 52%, 57%, and 96%, and late airway response (LAR) by 67%, 50%, and 79%, respectively. Orally administered with Asapiprant (5 mg/kg) for 4 days, the Asapiprant significantly (P<0.01) suppresses antigen-induced nasal resistance by 73% in sheep. Treatment with 3 and 30 mg/kg of Asapiprant in pigs significantly (P<0.01) suppresses nasal secretion by 53% and 72%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly (P<0.05) reduces airway hyper-responsiveness (AHR), infiltration of inflammatory cells, and mucin production in bronchoalveolar lavage fluid (BALF), although treatment with Asapiprant at 0.1 mg/kg does not have a significant effect on any responses[1]. |