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Product IntroductionBioactivity英文名: Fevipiprant描述: Fevipiprant (NVP-QAW039) 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂，KD 值为1.1 nM，IC50为0
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Product Introduction
Bioactivity
英文名: Fevipiprant
描述: Fevipiprant (NVP-QAW039) 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂，KD 值为1.1 nM，IC50为0.44 nM，能够引发人体嗜酸性粒细胞的形状变化。
体外活性: 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.[
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 32 mg/mL
关键字: IL-4 | inhibit | Inhibitor | bronchial asthma | QAW-039 | NVP-QAW-039 | Th2 cells | abdominal aortic aneurysm | Prostaglandin Receptor | Fevipiprant | orally active | QAW 039 | NVP-QAW 039
相关产品: CRTh2 antagonist 2 | AF64394 | 7-FluorotryptaMine HCl | CAY10786 | Grp94 Inhibitor-1 | Urotensin II, mouse TFA (9047-55-6 free base) | Benzyl nicotinate | LP-471756 | (2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid | MS21570
相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library
Bioactivity
英文名: Fevipiprant
描述: Fevipiprant (NVP-QAW039) 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂，KD 值为1.1 nM，IC50为0.44 nM，能够引发人体嗜酸性粒细胞的形状变化。
体外活性: 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.[
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 32 mg/mL
关键字: IL-4 | inhibit | Inhibitor | bronchial asthma | QAW-039 | NVP-QAW-039 | Th2 cells | abdominal aortic aneurysm | Prostaglandin Receptor | Fevipiprant | orally active | QAW 039 | NVP-QAW 039
相关产品: CRTh2 antagonist 2 | AF64394 | 7-FluorotryptaMine HCl | CAY10786 | Grp94 Inhibitor-1 | Urotensin II, mouse TFA (9047-55-6 free base) | Benzyl nicotinate | LP-471756 | (2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid | MS21570
相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library
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