产品描述: Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma |
靶点:
DP2:1.14 nM (Kd);GPR;ProstaglandinReceptor |
体外研究:
Fevipiprant (0-10 µM) inhibits the gene expression of IL-4, IL-3, IL-5, IL-8, CSF1, CSF2 in n in human Th2 cells induced by activated mast cell supernatants |
体内研究:
Fevipiprant (10 mg/kg; in the drinking water) reduces CaCl2-induced AAA (abdominal aortic aneurysm) formation in mouse. Animal Model: C57Bl/6 mice Dosage: 10 mg/kg Administration: In the drinking water Result: Efficiently reduced CaCl2-induced AAA formation with diminished elastin degradation, aortic macrophage infiltration, MPO accumulation and MCP-1 expression. |
参考文献:
1. Brightling C, et al. The pharmacology of the prostaglandin D2 receptor 2 (DP2) receptor antagonist, fevipiprant. Pulm Pharmacol Ther. 2021 Jun;68:102030. 2. Lee HY, et al. Blockade of thymic stromal lymphopoietin and CRTH2 attenuates airway inflammation in a murine model of allergic asthma. Korean J Intern Med. 2020 May;35(3):619-629. 3. Weintraub NL, et al. Role of prostaglandin D2 receptors in the pathogenesis of abdominal aortic aneurysm formation. Clin Sci (Lond). 2022 Mar 18;136(5):309-321. |
溶解性:
soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.345 ml |
11.726 ml |
23.452 ml |
5 mM |
0.469 ml |
2.345 ml |
4.69 ml |
10 mM |
0.235 ml |
1.173 ml |
2.345 ml |
50 mM |
0.047 ml |
0.235 ml |
0.469 ml |
|
注意: |
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