Varespladib

Modify Date: 2025-08-22 10:14:16

Varespladib Structure
Varespladib structure
Common Name Varespladib
CAS Number 172732-68-2 Molecular Weight 380.394
Density 1.3±0.1 g/cm3 Boiling Point 667.9±65.0 °C at 760 mmHg
Molecular Formula C21H20N2O5 Melting Point N/A
MSDS USA Flash Point 357.7±34.3 °C

 Use of Varespladib


LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.IC50 value: 7 nMTarget: sPLA2in vitro: 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. [2] 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. [2] 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. [3]in vivo: Ex 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. [2] 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. [2]

 Names

Name LY315920(Varespladib)
Synonym More Synonyms

 Varespladib Biological Activity

Description LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.IC50 value: 7 nMTarget: sPLA2in vitro: 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. [2] 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. [2] 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. [3]in vivo: Ex 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. [2] 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. [2]
Related Catalog
References

[1]. Draheim SE, et al. Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. J Med Chem. 1996 Dec 20;39(26):5159-75.

[2]. Snyder DW, 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. 1999 Mar;288(3):1117-24.

[3]. Hori Y, et al. Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 667.9±65.0 °C at 760 mmHg
Molecular Formula C21H20N2O5
Molecular Weight 380.394
Flash Point 357.7±34.3 °C
Exact Mass 380.137207
PSA 111.62000
LogP 2.45
Appearance of Characters white solid
Vapour Pressure 0.0±2.1 mmHg at 25°C
Index of Refraction 1.630
InChIKey BHLXTPHDSZUFHR-UHFFFAOYSA-N
SMILES CCc1c(C(=O)C(N)=O)c2c(OCC(=O)O)cccc2n1Cc1ccccc1
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 VarespladibBioassay

View more

Name: Inhibition of mouse group2X phospholipase A2 fluorimetric assay
Source: ChEMBL
Target: Group 10 secretory phospholipase A2
External Id: CHEMBL990837
Name: Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
Source: NCGC
Target: N/A
External Id: SERCaMPGLuc-p1-antagonist
Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
Name: Inhibition of human group2V phospholipase A2 fluorimetric assay
Source: ChEMBL
Target: Phospholipase A2 group V
External Id: CHEMBL990834
Name: Inhibition of mouse group2F phospholipase A2 fluorimetric assay
Source: ChEMBL
Target: Group IIF secretory phospholipase A2
External Id: CHEMBL990833
Name: Inhibition of human group2X phospholipase A2 fluorimetric assay
Source: ChEMBL
Target: Group 10 secretory phospholipase A2
External Id: CHEMBL990836
Name: Inhibition of mouse group2V phospholipase A2 fluorimetric assay
Source: ChEMBL
Target: Phospholipase A2 group V
External Id: CHEMBL990835
Name: Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ...
Source: NCGC
External Id: huntington-HTTAS8-p1-FF-overN
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 Synonyms

({3-[Amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl}oxy)acetic acid
Varespladib
N-(3,4-dimethoxyphenyl)-6,7-dimethoxyquinazolin-4-amine
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