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Fevipiprant

Cat. No. M8973
Fevipiprant Structure
Synonym:

NVP-QAW039

Size Price Availability Quantity
5mg USD 67.5  USD75 In stock
10mg USD 99  USD110 In stock
25mg USD 198  USD220 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Fevipiprant (QAW039) is a selective, potent, reversible competitive CRTh2 antagonist. NVP-QAW039 displayed high affinity for the human CRTh2 receptor (1.14 ± 0.44 nM) expressed in Chinese hamster ovary cells, the binding being reversible and competitive with the native agonist prostaglandin D2(PGD2). QAW039 was also a potent inhibitor of PGD2-induced cytokine release in human Th2 cells.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 426.41
Formula C19H17F3N2O4S
CAS Number 872365-14-5
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Pharmacokinetics, Safety, and Tolerability of Fevipiprant (QAW039), a Novel CRTh2 Receptor Antagonist: Results From 2 Randomized, Phase 1, Placebo-Controlled Studies in Healthy Volunteers.
Erpenbeck VJ, et al. Clin Pharmacol Drug Dev. 2016 Jul;5(4):306-13. PMID: 27310331.

Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.
Sykes DA, et al. Mol Pharmacol. 2016 May;89(5):593-605. PMID: 26916831.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Fevipiprant, NVP-QAW039 supplier, Prostaglandin Receptor, inhibitors

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