Fevipiprant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

缓慢解离的 CRTh2 拮抗剂，Kd 为 1.14 nM。

A slowly dissociating CRTh2 antagonist with Kd of 1.14 nM; shows a half-life of 14.4 minutes, >7-fold slower than AZD-1981; inhibits PGD2-stimulated human eosinophil shape change, importantly, retains its potency in the whole-blood shape-change assay relative to the isolated shape change assay; also is a potent inhibitor of PGD2-induced cytokine release in human Th2 cells.Asthma Phase 3 Clinical(In Vitro):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.(In Vivo):Fevipiprant (10 mg/kg; in the drinking water) reduces CaCl2-induced AAA (abdominal aortic aneurysm) formation in mouse.

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.

Fevipiprant (10 mg/kg; in the drinking water) reduces CaCl2-induced AAA (abdominal aortic aneurysm) formation in mouse. Animal Model:C57Bl/6 miceDosage: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.

NVP-QAW039 | QAW-039

GPCR/G Protein

Prostaglandin Receptor

CRTh2

Inflammation/Immunology

Asthma

872365-14-5

426.4095

C19H17F3N2O4S

>98% (HPLC)

DMSO: ≥ 32 mg/mL

O=C(O)CC1=C(C)N(CC2=CC=C(S(=O)(C)=O)C=C2C(F)(F)F)C3=NC=CC=C31

1H-Pyrrolo[2,3-b]pyridine-3-acetic acid, 2-methyl-1-[[4-(methylsulfonyl)-2-(trifluoromethyl)phenyl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years