产品说明书

Fevipiprant

Print
Chemical Structure| 872365-14-5 同义名 : NVP-QAW039;QAW039;NVP-QAW-039 QAW-039
CAS号 : 872365-14-5
货号 : A570568
分子式 : C19H17F3N2O4S
纯度 : 99%+
分子量 : 426.409
MDL号 : MFCD28963975
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(70.35 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Fevipiprant is a potent and selective CRTh2 (DP2) receptor antagonist with Ki value of 4nM in a human DP2 receptor scintillation proximity binding assay, and IC50 values of 0.4nM for in both isolated human eosinophil shape change assay and human whole blood eosinophil shape change assay. Fevipiprant dose-dependently antagonize PGD2-stimulated [35S]-GTPγS activation at human CRTh2 receptors expressed in membranes from CHO cells. It inhibited DK-PGD2 induced cytokine production, including IL-4, IL-5 and IL-13, with IC50 values of 3.1nM, 2.6nM and 1.4nM in human CD4+ Th2 cells.
作用机制 Fevipiprant could bind to CRTh2 receptor through competition with the native agonist PGD2.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.73mL

2.35mL

1.17mL

23.45mL

4.69mL

2.35mL
参考文献

[1]Sandham DA, Barker L, et al. Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma. ACS Med Chem Lett. 2017 Apr 25;8(5):582-586.

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