CAS 172732-68-2|Varespladib

Introduction：Basic information about CAS 172732-68-2|Varespladib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Varespladib BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

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	/
MSDS	USA	Flash Point	357.7±34.3 °C

Names

Name	LY315920(Varespladib)
Synonym	More Synonyms

Varespladib BiologicalActivity

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	Signaling Pathways >>Metabolic Enzyme/Protease >>PhospholipaseResearch Areas >>Inflammation/Immunology
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.

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

Signaling Pathways >>Metabolic Enzyme/Protease >>PhospholipaseResearch Areas >>Inflammation/Immunology

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

Synonyms

Acetic acid, 2-[[3-(2-amino-1,2-dioxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]-

({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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