Varespladib (LY315920)

Catalog No.S1110

Varespladib (LY315920) Chemical Structure

Molecular Weight(MW): 380.39

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

Size Price Stock Quantity  
In DMSO USD 260 In stock
USD 170 In stock
USD 270 In stock
USD 770 In stock
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3 Customer Reviews

  • After serum deprivation for 48 h (A) or 24 h (B) MDA-MB-231 cells were treated with recombinant hGX (10 nM) in serum-free medium containing 0.1% FAF BSA for 24 h (A) or 96 h (B) in the presence or absence of the sPLA2 inhibitor varespladib (Var) at a final concentration of 50 μM.

    Mol Cancer, 2013, 12(1):111.. Varespladib (LY315920) purchased from Selleck.

    Hepatic immune cell infiltration in Mmp2 −/− mice administered the pan-sPLA 2 inhibitor varespladib (10 mg/kg per day, gavage, for 5 days). Collagenase-treated and liberated cells were surface-stained for indicated markers (A) and quantitated. n=3 WT and n=5 Mmp2 −/−. *P≤0.05 vs WT untreated. † P≤0.05 vs Mmp2 −/− untreated. MHC II, major histocompatibility complex II; sPLA2, secreted phospholipase A2; SSC, Side-scattered light (a magnitude proportional to cell granularity or internal complexity); WT, wild type.

    J Am Heart Assoc, 2015, 4:e002553.. Varespladib (LY315920) purchased from Selleck.

  • Cells were treated with inhibitors for cPLA2α (5 μM Inhibitor 28, 1 μM CAY10502, 5 μM AVX002, 5 μM ATK); sPLA2 (10 μM CAY10590, 10 μM Varespladib) or COX1/2 (10 μM Indomethasin) for 2 hours followed by FSL-1 (100 ng/mL) or Pam3CSK4 (200 ng/mL) for 24 hours. Release of PGE2 was measured by ELISA. Results shown are mean ± SD of three independent experiments.

    PLoS One, 2015, 10(4):e0119088.. Varespladib (LY315920) purchased from Selleck.

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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

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 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]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: Transgenic Mice Expressing Human sPLA2 Protein.
  • Formulation: LY315920 is dissolved in 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300.
  • Dosages: ≤3 mg/kg
  • Administration: Administered via i.v. and p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.39
Formula

C21H20N2O5

CAS No. 172732-68-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01522196 Terminated Sickle Cell Disease|Vaso-occlusive Crisis Anthera Pharmaceuticals February 2012 Phase 2
NCT01359605 Completed Healthy Volunteers Anthera Pharmaceuticals June 2011 Phase 1
NCT01359579 Terminated Renal Impairment Anthera Pharmaceuticals June 2011 Phase 1
NCT01130246 Terminated Acute Coronary Syndrome Anthera Pharmaceuticals May 2010 Phase 3
NCT00743925 Completed Acute Coronary Syndrome Anthera Pharmaceuticals July 2008 Phase 2
NCT00533039 Completed Coronary Artery Disease University Health Network, Toronto|Anthera Pharmaceuticals October 2007 Phase 2

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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.

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Phospholipase (e.g. PLA) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID