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LY315920

Cat. No. M1935

LY315920 Structure

Synonym: Varespladib

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 640 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY315920 (Varespladib) is a potent and selective secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM. LY315920 inhibited sPLA2 activity with an IC50 of 9 +/- 1 nM or 7.3 x 10(-6) mole fraction, which approached the stiochiometric limit of this assay in a chromogenic isolated enzyme assay. LY315920 (Varespladib) was 40-fold less active against human, group IB, pancreatic sPLA2 and was inactive against cytosolic PLA2 and the constitutive and inducible forms of cyclooxygenase. The i.v. administration of LY315920, 5 min before harvesting the bronchoalveolar lavage cells, resulted in the inhibition of sPLA2-induced production of TXA2 with an ED50 of 16.1 mg/kg. LY315920 (Varespladib) is currently undergoing clinical evaluation and should help to define the role of sPLA2 in various inflammatory disease states.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Transgenic Mice Expressing Human sPLA2 Protein
Formulation 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300 in water
Dosages 0.3–3 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 380.39
Formula C21H20N2O5
CAS Number 172732-68-2
Purity >99%
Solubility DMSO 75 mg/mL
Storage at -20°C
References

Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI.
Snyder DW, et al. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24. PMID: 10027849.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY315920, Varespladib supplier, Phospholipase, inhibitors

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