Fevipiprant

SKU: orb1303505

Description

Fevipiprant (NVP-QAW039) is a potent and selective reversible antagonist of the CRTh2 receptor. It is a valuable research tool for investigating allergic diseases, such as asthma and atopic dermatitis, in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 872365-14-5
• MW: 426.41
• Purity: 99.59% (May vary between batches)
• Formula: C₁₉H₁₇F₃N₂O₄S
• SMILES: Cc1c(CC(O)=O)c2cccnc2n1Cc1ccc(cc1C(F)(F)F)S(C)(=O)=O
• Target: GPCR,Prostaglandin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.69 mM);DMSO:60 mg/mL (140.71 mM)

Bioactivity

• Target IC50:
  DP2:1.14 nM (Kd)|CRTH2:0.44 nM
• 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.[

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ProstaglandinReceptor, Prostaglandin Receptor, QAW 039, QAW039, QAW-039, Th2 cells, bronchial asthma, abdominal aortic aneurysm, CRTh2, Fevipiprant, NVP-QAW 039, NVP-QAW039, NVP-QAW-039, orally active, inhibit, IL-4, Inhibitor

Compound Identifiers

PubChem CID

23582412