S-555739 - Names and Identifiers
S-555739 - Physico-chemical Properties
Molecular Formula | C24H27N3O7S
|
Molar Mass | 501.55 |
Density | 1.341±0.06 g/cm3(Predicted) |
Melting Point | >218°C (dec.) |
Boling Point | 731.6±70.0 °C(Predicted) |
Solubility | DMSO : 11.11 mg/mL (22.15 mM; Need ultrasonic) |
Appearance | Solid |
Color | White to Off-White |
pKa | 2.92±0.10(Predicted) |
Storage Condition | -20°C Freezer, Under inert atmosphere |
Use | Asapiprant is a potent and selective DP1 receptor antagonist with a Ki value of 0.44 nM. |
S-555739 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 1.994 ml | 9.969 ml | 19.938 ml |
5 mM | 0.399 ml | 1.994 ml | 3.988 ml |
10 mM | 0.199 ml | 0.997 ml | 1.994 ml |
5 mM | 0.04 ml | 0.199 ml | 0.399 ml |
Last Update:2024-01-02 23:10:35
S-555739 - In Vivo
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。
Last Update:2023-08-16 21:32:38