Varespladib ( LY315920 )

Catalog No. M12623 CAS No. 172732-68-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

Varespladib
Note

Research use only, not for human use.
Brief Description

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

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

Western Blot Analysis Cell Line:HCjE cells Concentration:10 μM Incubation Time:24 hours and 48 hours Result:Significantly inhibited the RA-induced MUC16 protein expression at both time points.RT-PCR Cell Line:HCjE cells Concentration:10 μ Incubation Time:24 hours and 48 hours Result:Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
In Vivo

Animal Model:Male Hartley guinea pigs (300-500 g) Dosage:3 mg/kg, 10 mg/kg, and 30 mg/kg Administration:Intravenous injection (Pharmacokinetic study)Result:Consistent inhibition of sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.
Synonyms

LY315920
Pathway

Metabolic Enzyme/Protease
Target

Phospholipase
Recptor

hnsPLA2
Research Area

Inflammation/Immunology
Indication

——

CAS Number

172732-68-2
Formula Weight

380.39
Molecular Formula

C21H20N2O5
Purity

>98% (HPLC)
Solubility

DMSO: 76 mg/mL (199.79 mM)
SMILES

NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O
Chemical Name

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

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

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