Varespladib

≥98% (HPLC), Secretory phospholipase A2 inhibitor, powder

Sinônimo(s):

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

Sobre este item

Fórmula empírica (Notação de Hill):

C₂₁H₂₀N₂O₅

Número CAS:

172732-68-2

Peso molecular:

380.39

UNSPSC Code:

41106300

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Propriedades

Nome do produto

Varespladib, ≥98% (HPLC)

Quality Segment

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

−20°C

SMILES string

[Na+].[n]2(c3c(c(ccc3)OCC(=O)[O-])c(c2CC)C(=O)C(=O)N)Cc1ccccc1

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

Descrição

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[1]

• to test its neutralization functionality on the black snake species  collettivenom[2]

• in combination with snake venom metalloproteinases (SVMP)-inhibitor, marimastat to test its protective functionality on envenoming by vipers[3]

Biochem/physiol Actions

Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2).

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.[3] 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.[4]