Fevipiprant 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂，KD值为1.1 nM，IC50为0.44 nM，能够引发人体嗜酸性粒细胞的形状变化。

Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.

CRTh2-mediated shape change in eosinophils was used to profile QAW039 in whole blood and represents a physiologically relevant environment. The comparable IC50 values for QAW039 in the whole blood and isolated shape-change assays are consistent with its lower plasma-protein binding and its relatively slow dissociation kinetics that drive its increased potency .QAW039 is highly potent in whole-blood systems, with the IC50 value obtained consistent with the affinity values calculated from radioligand experiments. In a further disease-relevant cellular context, the potency of QAW039 in the isolated Th2 cell cytokine inhibition assay is consistent with its CRTh2 receptor affinity, and, as with eosinophil assay readouts, this represents an improved potency compared with QAV680.[

872365-14-5

C19H17F3N2O4S

426.41

NVP-QAW039;非维匹仑;QAW039

DMSO:32 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years