An antagonist of DP1 (Ki = 0.44 nM); selective for DP1 over DP2

Asapiprant – 5 mg

Brand:
Cayman
CAS:
932372-01-5
Storage:
-20
UN-No:
Non-Hazardous - /

Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).{50862} 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.  

 

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SKU: 30008 - 5 mg Category:

Description

An antagonist of DP1 (Ki = 0.44 nM); selective for DP1 over DP2, as well as the TXA2, PGI2, and PGE1-4 receptors (Kis = >5,000, >4,800, >6,300, 120->6,600 nM, respectively); reduces PGD2-induced increases in nasal resistance in a guinea model of allergic rhinitis at 1 and 3 mg/kg; reduces nasal secretion at 3 and 30 mg/kg and antigen-induced cell infiltration at 3 and 10 mg/kg in a guinea pig model of ovalbumin-induced allergic rhinitis; decreases airway hyperresponsiveness, inflammatory cell infiltration in 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

Synonyms:  S-555739

Molecular weight: 501.6

CAS: 932372-01-5

Purity: ≥98%

Formulation: A solid

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