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Fevipiprant

Catalog No. T3965   CAS 872365-14-5
Synonyms: QAW039, NVP-QAW039

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

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Fevipiprant, CAS 872365-14-5
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 72.00
25 mg In stock $ 147.00
50 mg In stock $ 228.00
100 mg In stock $ 372.00
200 mg In stock $ 549.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.32%
Purity: 98%
Purity: 98%
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Biological Description
Chemical Properties
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 QAW039, 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 )

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:
Drug Repurposing Compound Library Target-Focused Phenotypic Screening Library Anti-Obesity Compound Library Bioactive Compound Library Inhibitor Library ReFRAME Related Library Bioactive Compounds Library Max Clinical Compound Library GPCR Compound Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets
Fezagepras sodium CRTh2 antagonist 2 FL104 BTB09089 GPR35 agonist 2 GLPG1205 BMS-903452 TUG-770

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Keywords

Fevipiprant 872365-14-5 Endocrinology/Hormones GPCR/G Protein Immunology/Inflammation GPR Prostaglandin Receptor IL-4 inhibit Inhibitor bronchial asthma QAW039 Th2 cells QAW 039 abdominal aortic aneurysm QAW-039 orally active NVP-QAW039 inhibitor