1. GPCR/G Protein
    Immunology/Inflammation
  2. CRTH2 (GPR44)

Fevipiprant (Synonyms: NVP-QAW039; QAW039)

Cat. No.: HY-16768 Purity: 98.31%
Data Sheet SDS Handling Instructions

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood.

For research use only. We do not sell to patients.
Fevipiprant Chemical Structure

Fevipiprant Chemical Structure

CAS No. : 872365-14-5

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100 mg $440 In-stock
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Description

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood. IC50:0.44 nM(PGD2-induced eosinophil shape change) Kd value:1.1nM(CRTh2 receptor)[1] In vitro: 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[2].

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References
Molecular Weight

426.41

Formula

C₁₉H₁₇F₃N₂O₄S

CAS No.

872365-14-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 32 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Fevipiprant
Cat. No.:
HY-16768
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