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SML1100

Sigma-Aldrich

Varespladib

≥98% (HPLC)

Synonym(s):

2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-acetic acid, A-001, LY-315920, LY315920

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About This Item

Empirical Formula (Hill Notation):
C21H20N2O5
CAS Number:
Molecular Weight:
380.39
UNSPSC Code:
41106300
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

−20°C

InChI

1S/C21H20N2O5.Na/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);/q;+1/p-1

InChI key

XZZUHXILQXLTGV-UHFFFAOYSA-M

Application

Varespladib has been used as a secretory phospholipase A (sPLA2) inhibitor:
  • to test its effect on the human astrocytes subjected to psychosine-induced toxicity
  • to test its neutralization functionality on the black snake species P. colletti venom
  • in combination with snake venom metalloproteinases (SVMP)-inhibitor, marimastat to test its protective functionality on envenoming by vipers

Biochem/physiol Actions

Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V, and X enzymes at low nM concentrations.
Varespladib is effective against viper and elapid venoms and is used in snakebite therapy. It is reported to interact with the hydrophobic channel of the PLA2-like toxin in in vitro structural studies. It blocks inflammatory cascades related to the sPLA2.

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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Cedric Misslin et al.
PloS one, 12(11), e0187217-e0187217 (2017-11-03)
Krabbe disease is a fatal rare inherited lipid storage disorder affecting 1:100,000 births. This illness is caused by mutations in the galc gene encoding for the enzyme galactosylceramidase (GALC). Dysfunction of GALC has been linked to the toxic build-up of

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