Varespladib

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

Varespladib (LY315920) 是一种有效的选择性人非胰腺分泌型磷脂酶 A2 (hnsPLA) 抑制剂，IC50 为 7 nM。

Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3.

Western Blot Analysis Cell Line:HCjE cells Concentration:10 μM Incubation Time:24 hours and 48 hours Result:Significantly inhibited the RA-induced MUC16 protein expression at both time points.RT-PCR Cell Line:HCjE cells Concentration:10 μ Incubation Time:24 hours and 48 hours Result:Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.

Animal Model:Male Hartley guinea pigs (300-500 g) Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg Administration:Intravenous injection (Pharmacokinetic study)Result:Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.

LY315920

Metabolic Enzyme/Protease

Phospholipase

hnsPLA2

Inflammation/Immunology

——

172732-68-2

380.39

C21H20N2O5

>98% (HPLC)

DMSO: 76 mg/mL (199.79 mM)

NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O

2-((3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yl)oxy)acetic acid

(-20℃)

With Ice Pack

≥ 2 years