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Fevipiprant

Catalog No. T3965 CAS 872365-14-5

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

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Fevipiprant, CAS 872365-14-5

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist.
Targets&IC50	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.[

Synonyms	IL-4, inhibit, Inhibitor, bronchial asthma, Fevipiprant, QAW039, Th2 cells, QAW 039, abdominal aortic aneurysm, Prostaglandin Receptor, QAW-039, orally active, NVP-QAW039
Molecular Weight	426.41
Formula	C19H17F3N2O4S
CAS No.	872365-14-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

1. Sykes DA, et al. Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy. Mol Pharmacol. 2016 May;89(5):593-605. 2. Erpenbeck VJ, rt al. Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo-Controlled Studies in Healthy Volunteers. Clin Pharmacol Drug Dev. 2016 Jul;5(4):306-13.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Immunology/Inflammation Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.