Fevipiprant
Cat. No. :YN321092
CAS No. :872365-14-5
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Product Name: | Fevipiprant |
CAS NO.: | 872365-14-5 |
Chemical Name: | |
Synonyms: | |
Molecular Weight: | 426.41 |
Molecular Formula: | C₁₉H₁₇F₃N₂O₄S |
SMILES: | O=C(O)CC1=C(C)N(CC2=CC=C(S(=O)(C)=O)C=C2C(F)(F)F)C3=NC=CC=C31 |
Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
Transportation: | Room temperature in continental US; may vary elsewhere. |
Description: | Fevipiprant (QAW039; NVP-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 0.44nM for inhibition of PGD2-induced eosinophil shape change in human whole blood. IC50:0.44nM(PGD2-induced eosinophil shape change) Kd value:1.1nM(CRTh2 receptor) 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 radiolig and 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. |
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References: |
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