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.
Cited by 6 Publications
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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.
Purity & Quality Control
Choose Selective Phospholipase (e.g. PLA) Inhibitors
|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.|
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. 
|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.  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. |
|In vitro||DMSO||76 mg/mL (199.79 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
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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|
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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