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Fevipiprant

CAS号

872365-14-5

分子式

C19H17F3N2O4S

主要靶点

GPR|Prostaglandin Receptor

仅限科研使用

Cat No : CM03600

Print datasheet

Synonyms

Inhibitor|orally active|NVP-QAW 039|NVP-QAW039|NVP-QAW-039|Prostaglandin Receptor|ProstaglandinReceptor|QAW 039|QAW039|QAW-039|非维匹仑|Th2 cells|abdominal aortic aneurysm|bronchial asthma|Fevipiprant|inhibit|IL-4|CRTh2

验证数据展示

  • CAS No.: 872365-14-5

    Fevipiprant
    CAS#: 872365-14-5

产品信息

CAS号 872365-14-5
分子式 C19H17F3N2O4S
主要靶点 GPR|Prostaglandin Receptor
主要通路 G 蛋白偶联受体|内分泌与激素|免疫与炎症|G 蛋白偶联受体
分子量 426.41
纯度 99.59%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|orally active|NVP-QAW 039|NVP-QAW039|NVP-QAW-039|Prostaglandin Receptor|ProstaglandinReceptor|QAW 039|QAW039|QAW-039|非维匹仑|Th2 cells|abdominal aortic aneurysm|bronchial asthma|Fevipiprant|inhibit|IL-4|CRTh2

靶点活性

CRTH2:0.44 nM

体外活性

CRTh2介导的嗜酸性粒细胞形状变化被用于在全血环境下对Fevipiprant的特性进行评估，这一过程模拟了生理环境中的实际情况。Fevipiprant在全血系统中和单独的形状变化实验中得到的相似IC50值，显示了其较低的血浆蛋白结合能力和相对缓慢的解离动力学，这些都促使了其更高的药效。Fevipiprant在全血系统中表现出极高的活性，其IC50值与放射配体实验计算得到的亲和力值一致。在进一步与疾病相关的细胞环境中，Fevipiprant在孤立的Th2细胞细胞因子抑制实验中的药效，与其CRTh2受体的亲和力保持一致，与嗜酸性粒细胞实验结果一样，与QAV680相比，显示出了改善的药效。

溶解度

DMSO:60 mg/mL (140.71 mM)

参考文献

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.

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