An antagonist of DP1
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Asapiprant

Item No. 30008

Safety Data Sheet (SDS) (PDF)
Technical Information
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
Purity
≥98%
Formulation
A solid
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 3 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Asapiprant is an antagonist of the prostaglandin D1 (PGD1) receptor (DP1; Ki = 0.44 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takahashi, G., Asanuma, F., Suzuki, N., et alEffect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur. J. Pharm. 765(15), 15-23 (2015).