Inhibitor of group IIA, IIE, and X forms of sPLA2
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LY315920

Item No. 18267

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[3-(2-amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-acetic acid
CAS Number
172732-68-2
Synonyms
  • ​Varespladib
Molecular Formula
C21H20N2O5
Formula Weight
380.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 3 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
217, 256, 331 nm
SMILES
O=C(O)COC1=C2C(N(CC3=CC=CC=C3)C(CC)=C2C(C(N)=O)=O)=CC=C1
InChi Code
InChI=1S/C21H20N2O5/c1-2-14-19(20(26)21(22)27)18-15(9-6-10-16(18)28-12-17(24)25)23(14)11-13-7-4-3-5-8-13/h3-10H,2,11-12H2,1H3,(H2,22,27)(H,24,25)
InChi Key
BHLXTPHDSZUFHR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $178

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    25 mg

    $417

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    50 mg

    $701

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    Product Description

    LY315920 is an inhibitor of human group IIA (hGIIA) secretory phospholipase A2 (sPLA2; IC50 = 9 nM).1 It also potently inhibits human GIIE and GX isoforms, as well as the corresponding mouse isoforms, but poorly inhibits other PLA2 enzymes.1,2,3,4 LY315920 inhibits sPLA2-induced release of thromboxane A2 from isolated guinea pig lung bronchoalveolar lavage cells (IC50 = 0.79 µM).2 Intravenous or oral administration of LY315920 to transgenic mice expressing human sPLA2 inhibits serum sPLA2 activity in a dose-related manner over four hours.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Draheim, S.E., Bach, N.J., Dillard, R.D., et al. Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. J. Med. Chem. 39(26), 5159-5175 (1996).

    2. Snyder, D.W., Bach, N.J., Dillard, R.D., et al. 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. J. Pharmacol. Exp. Ther. 288(3), 1117-1124 (1999).

    3. Oslund, R.C., Cermak, N., and Gelb, M.H. Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2. J. Med. Chem. 51(15), 4708-4714 (2008).

    4. Smart, B.P., Pan, Y.H., Weeks, A.K., et al. Inhibition of the complete set of mammalian secreted phospholipases A2 by indole analogues: A structure-guided study. Bioorg. Med. Chem. 12(7), 1737-1749 (2004).