Varespladib (LY315920)

Catalog No.S1110

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

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Varespladib (LY315920) Chemical Structure

Varespladib (LY315920) Chemical Structure
Molecular Weight: 380.39

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Varespladib (LY315920) is available in the following compound libraries:

Product Information

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Product Description

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.
Targets hnsPLA2 [1]
IC50 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]
Features A potent and selective secretory phospholipase A2 inhibitor.

Protocol(Only for Reference)

Kinase Assay: [1]

DOC/PC Phospholipase A2 Inhibition Assay Aliquots of 10 μL of LY315920 solutions in DMSO are added to 20 μL (10 ng) of enzyme in 25 mM Tris.HCl (pH 8) with 0.25 mg/mL BSA and 150 μL of assay buffer containing 50mM Tris (pH 8), 0.2 M NaCl, 2 mM CaCl2, and 1 mg/mL fatty acid free BSA. To each tube is added 20 μL of a freshly prepared, iced stock solution of the PC and bile salt, which have been sonicated and concocted such that the final 200 μL reaction volume would contain 3 mM DOC/1 mM total PC and approximately 1 × 105 cpm of [14C]PC. To prepare the lipid substrate, aliquots of labeled PC (1-palmitoyl-2[14C]-oleoylphosphatidyl choline) and 100 mM stock cold PC in chloroform, and 100 mM DOC (sodium salt of deoxycholic acid) in ethanol are mixed, dried under a N2 stream, and then reconstituted in 10 mM Tris with 0.2 mM NaCl, before sonicating for 10 minutes. The assay tubes are incubated for 1 hour in a 40 °C water bath. The reaction is stopped with 1.5 mL of Doles 2-propanol/heptane/0.5 M H2SO4 at 40:10:1 (v/v) with 1 mg/mL palmitic acid. The mixtures are then heated for 1 minute at 60 °C before 1 mL of H2O and 1.25 mL of heptane are added and mixed thoroughly. After the two phases are allowed to separate, the upper phase is transferred to 1 mL of heptane containing 150 mg of dried silica and mixed again before centrifugation for 5 minutes at 1500 g. The supernatant is removed for scintillation counting of the liberated [14C]oleic acid. The degree of inhibition is compared to diluent controls, and the inhibitory concentrations are calculated.

Animal Study: [2]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Draheim SE, et al. J Med Chem. 1996, 39(26), 5159-5175.

[2] Snyder DW, et al. J Pharmacol Exp Ther. 1999, 288(3), 1117-1124.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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

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Chemical Information

Download Varespladib (LY315920) SDF
Molecular Weight (MW) 380.39
Formula

C21H20N2O5

CAS No. 172732-68-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 76 mg/mL (199.79 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yloxy)acetic acid

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.

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