A DP2/CRTH2 antagonist
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Fevipiprant

Item No. 20263

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methyl-1-[[4-(methylsulfonyl)-2-(trifluoromethyl)phenyl]methyl]-1 H -pyrrolo[2,3b]pyridine-3-acetic acid
CAS Number
872365-14-5
Synonyms
  • NVP-QAW039
  • QAW039
Molecular Formula
C19H17F3N2O4S
Formula Weight
426.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMF:PBS(pH7.2) (1:2): 0.33 mg/mLDMSO: 10 mg/mLEthanol: 1 mg/mL
λmax
224, 291 nm
SMILES
CS(C1=CC=C(CN2C(C)=C(CC(O)=O)C3=C2N=CC=C3)C(C(F)(F)F)=C1)(=O)=O
InChi Code
InChI=1S/C19H17F3N2O4S/c1-11-15(9-17(25)26)14-4-3-7-23-18(14)24(11)10-12-5-6-13(29(2,27)28)8-16(12)19(20,21)22/h3-8H,9-10H2,1-2H3,(H,25,26)
InChi Key
GFPPXZDRVCSVNR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $63

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    1 mg

    $118

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    5 mg

    $514

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    Product Description

    Fevipiprant is a DP2/CRTH2 antagonist (Ki = 1.05 nM).1 It reduces shape change of eosinophils induced by prostaglandin D2 (PGD2; Item No. 12010) with IC50 values of 0.4 and 0.44 nM for isolated human eosinophils and human whole blood, respectively. Fevipiprant inhibits PGD2-induced release of IL-5 and IL-13 in isolated human CD4+ Th2 cells (IC50s = 2.56 and 1.4 nM, respectively). It reduces the number of eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of asthma (ED50 = ~1 mg/kg).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sykes, D.A., Bradley, M.E., Riddy, D.M., et al. Fevipiprant (QAW039), a slowly dissociating CRTh2 antagonist with the potential for improved clinical efficacy. Mol. Pharmacol. 89(5), 593-605 (2016).

    2. Sandham, D., Asano, K., Barker, L., et al. Fevipiprant, a potent selective prostaglandin D2 receptor 2 (DP2) antagonist, dose-dependently inhibits pulmonary inflammation in a mouse model of asthma. Am. J. Respir. Crit. Care Med. 197, A1418 (2018).