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Varespladib(LY 315920)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Varespladib(LY 315920)图片
CAS NO:172732-68-2
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)380.39
FormulaC21H20N2O5
CAS No.172732-68-2(Varespladib);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 76 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SynonymsA002; A 002; LY315920; Varespladib; LY-315920; LY 315920; A-002;

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

InChi Key: BHLXTPHDSZUFHR-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H20N2O5/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25)

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

实验参考方法
In Vitro

In vitro activity: LY315920 exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. In BAL cells challenged with human sPLA2, LY315920 at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. In human conjunctival epithelial cell line (HCjE), LY315920 (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours.


Kinase Assay: Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.


Cell Assay: In BAL cells challenged with human sPLA2, Varespladib at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. In human conjunctival epithelial cell line (HCjE), Varespladib (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours.

In VivoEx vivo, LY315920 at doses ranging from 3 mg/kg to 30 mg/kg via i.v. inhibits human sPLA2-induced release of thromboxane from guinea pig BAL cells with ED50 of 16.1 mg/kg. In Transgenic Mice Expressing Human sPLA2, both oral and i.v. administration of LY315920 (0.3 mg/kg–3 mg/kg) abolishes serum sPLA2 activity in a dose and time dependent manner.
Animal modelTransgenic Mice Expressing Human sPLA2 Protein
Formulation & DosageDissolved in 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300.; ≤3 mg/kg; Oral gavage or i.v.
ReferencesJ Med Chem. 1996 Dec 20;39(26):5159-75; J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.