Asapiprant
Asapiprant is a potent and selective DP1 receptor antagonist, with a Ki of 0.44 nM. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. Treatment with Asapiprant in rats at 10mg/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. In addition, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. These results show that asapiprant is a potent and selective DP1 receptor antagonist, and exerts suppressive effects in the animal models of allergic diseases.
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Chemical Information
| Name | Asapiprant |
|---|---|
| Iupac Chemical Name | 2-(5-(4-((4-Isopropoxyphenyl)sulfonyl)piperazin-1-yl)-2-(oxazol-2-yl)phenoxy)acetic acid |
| Synonyms | Asapiprant,S-555739; S 555739; S555739 |
| Molecular Formula | C24H27N3O7S |
| Molecular Weight | 501.55 |
| Smile | C(C)(C)OC1=CC=C(C=C1)S(=O)(=O)N1CCN(CC1)C=1C=CC(=C(OCC(=O)O)C1)C=1OC=CN1 |
| InChiKey | ZMZNWNTZRWXTJU-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 932372-01-5 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid to white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO, not in water |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma.
Takahashi G, et al. Eur J Pharmacol. 2015 Oct 15;765:15-23. PMID: 26277322.
Chemical Structure
