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    Varespladib (LY 315920)
    Varespladib (LY 315920)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0839
    CAS #: 172732-68-2 Purity ≥98%

    Description: Varespladib (formerly A-002; A 002; LY315920; LY-315920) is a investigational drug with the potential for treating inflammatory diseases such as acute coronary syndrome and acute chest syndrome as well as snakebite. It works as s selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. 

    References: J Med Chem. 1996 Dec 20;39(26):5159-75; J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.

    Related CAS: 172733-42-5 (Varespladib Sodium); 172733-08-3 [Varespladib Methyl (A-002; LY-333013; S-3013)]

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    Molecular Weight (MW)380.39
    FormulaC21H20N2O5
    CAS No.172732-68-2(Varespladib);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 76 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    SynonymsA002; A 002; LY315920; Varespladib; LY-315920; LY 315920; A-002; 

    Chemical Name: 2-((3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-indol-4-yl)oxy)acetic acid

    InChi Key: BHLXTPHDSZUFHR-UHFFFAOYSA-N

    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)

    SMILES Code: NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM. 


    Cell Assay: In BAL cells challenged with human sPLA2, Varespladib 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), Varespladib (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 VivoEx 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.
    Animal modelTransgenic Mice Expressing Human sPLA2 Protein
    Formulation & DosageDissolved in 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300.; ≤3 mg/kg; Oral gavage or i.v.
    ReferencesJ Med Chem. 1996 Dec 20;39(26):5159-75; J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Varespladib (LY315920)

    Inhibition of human sPLA2-induced release of thromboxane from guinea pig BAL cells by LY315920 (0.1–3 μM) in vitro.


    Varespladib (LY315920)
    Lack of inhibitory effect of LY315920 (3 μM) on arachidonic acid-induced thromboxane generation from guinea pig BAL cells. Indomethacin (10 μM) was used as a positive control. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.
     

    Varespladib (LY315920)

    LY315920 administered i.v. inhibited human sPLA2-induced release of thromboxane from guinea pig BAL cells.


    Varespladib (LY315920)

    Effect of LY315920 (10 μM) on contractile responses induced by arachidonic acid on guinea pig lung pleural strips. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.
     

    Varespladib (LY315920)

    Effect of i.v. (A) and oral (B) administration of LY315920 (0.3–3 mg/kg) or vehicle on sPLA2 enzyme activity in serum of transgenic animals expressing the human sPLA2protein. J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.


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