Home Metabolism Phospholipase (e.g. PLA) inhibitor Varespladib (LY315920) For research use only.

Varespladib (LY315920)

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

Varespladib (LY315920) Chemical Structure

Varespladib (LY315920) Chemical Structure

CAS No. 172732-68-2

Purity & Quality Control

Varespladib (LY315920) Related Products

Signaling Pathway

Phospholipase (e.g. PLA) Signaling Pathways

Phospholipase (e.g. PLA) Signaling Pathway

Biological Activity

Description Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3.
Features A potent and selective secretory phospholipase A2 inhibitor.
Targets
hnsPLA2 [1]
(Cell-free assay)
7 nM
In vitro
In vitro 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. [2] 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. [2] 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. [3]
In Vivo
In vivo Ex 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. [2] 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. [2]
Animal Research Animal Models Transgenic Mice Expressing Human sPLA2 Protein.
Dosages ≤3 mg/kg
Administration Administered via i.v. and p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01359605 Completed
Healthy Volunteers
Anthera Pharmaceuticals
 June 2011 Phase 1
NCT01359579 Terminated
Renal Impairment
Anthera Pharmaceuticals
 June 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 380.39 Formula

C21H20N2O5
CAS No. 172732-68-2 SDF Download Varespladib (LY315920) SDF
Smiles CCC1=C(C2=C(N1CC3=CC=CC=C3)C=CC=C2OCC(=O)O)C(=O)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (199.79 mM) Warmed with 50°C water bath; Ultrasonicated; Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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