[CAS NO. 172732-68-2] Varespladib

Name: Varespladib
Brand: Arctom Scientific
SKU: HY-13402

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PRODUCTS SPECIFICATIONS [172732-68-2]

Distributor

Catalog

HY-13402

Brand

MCE

CAS

172732-68-2

DESCRIPTION [172732-68-2]

Overview

MDL	-
Molecular Weight	380.39
Molecular Formula	C21H20N2O5
SMILES	O=C(O)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A ₂ (sPLA ₂ ) inhibitor with an IC ₅₀ of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC ₅₀ s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively ^[1] .

IC50 & Target

sPLA2

9 nM (IC ₅₀ )

In Vitro

Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment results in complete inhibition of the RA-induced increase in MUC16 protein detected in cell lysates at both time points ^[2] .
Varespladib (10 μM; 24 and 48 hours; HCjE cells) treatment significantly inhibits RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis ^[2]

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 ^[2]

Cell Line:	HCjE cells
Concentration:	10 μM
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

Varespladib treatment inhibits human sPLA ₂ -induced release of thromboxane A ₂ (TXA ₂ ) from isolated guinea pig lung bronchoalveolar lavage cells with an IC ₅₀ of 0.79 μM. And the ED ₅₀ for Varespladib is 16.1 mg/kg ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Hartley guinea pigs (300-500 g) ^[1]
Dosage:	3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:	Intravenous injection (Pharmacokinetic study)
Result:	Consistent inhibition of sPLA ₂ activity in BAL fluid was observed. Reduced the human sPLA ₂ -induced generation of TXA ₂ on BAL cells from guinea pigs.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01359605	Anthera Pharmaceuticals	Healthy Volunteers	June 2011	Phase 1
NCT00743925	Anthera Pharmaceuticals	Acute Coronary Syndrome	July 2008	Phase 2
NCT01359579	Anthera Pharmaceuticals	Renal Impairment	June 2011	Phase 1
NCT01522196	Anthera Pharmaceuticals	Sickle Cell Disease\|Vaso-occlusive Crisis	February 2012	Phase 2
NCT04996264	Ophirex, Inc.\|Premier Research Group plc	Snakebites\|Envenoming\|Envenoming, Snake\|Envenomation, Snake	August 15, 2021	Phase 2
NCT00533039	University Health Network, Toronto\|Anthera Pharmaceuticals	Coronary Artery Disease	October 2007	Phase 2
NCT01130246	Anthera Pharmaceuticals	Acute Coronary Syndrome	May 2010	Phase 3
NCT04969991	Ophirex, Inc.\|Premier Research Group plc	Coronavirus Disease 2019\|Disease Caused by Severe Acute Respiratory Syndrome Coronavirus 2	June 30, 2021	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 262.89 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6289 mL	13.1444 mL	26.2888 mL
5 mM	0.5258 mL	2.6289 mL	5.2578 mL
10 mM	0.2629 mL	1.3144 mL	2.6289 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 2.5 mg/mL (6.57 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 17% Polyethylene glycol 12-hydroxystearate in saline

Solubility: 1.5 mg/mL (3.94 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

Synonyms

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

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

2-[[3-(2-Amino-2-oxoacetyl)-2-ethyl-1-(phenylmethyl)-1H-indol-4-yl]oxy]acetic acid

LY 315920

Varespladib

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