1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. Varespladib

Varespladib (Synonyms: LY315920)

Cat. No.: HY-13402 Purity: 98.68%
Handling Instructions

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 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 IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

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

Varespladib Chemical Structure

Varespladib Chemical Structure

CAS No. : 172732-68-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 79 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 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 IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively[1].

IC50 & Target[1]

sPLA2

9 nM (IC50)

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 sPLA2-induced release of thromboxane A2 (TXA2) from isolated guinea pig lung bronchoalveolar lavage cells with an IC50 of 0.79 μM. And the ED50 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 sPLA2 activity in BAL fluid was observed. Reduced the human sPLA2-induced generation of TXA2 on BAL cells from guinea pigs.
Clinical Trial
Molecular Weight

380.39

Formula

C₂₁H₂₀N₂O₅

CAS No.
SMILES

O=C(O)COC1=CC=CC2=C1C(C(C(N)=O)=O)=C(CC)N2CC3=CC=CC=C3

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 : ≥ 32 mg/mL (84.12 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VarespladibLY315920LY 315920LY-315920PhospholipaseRecombinanthumangroupIIAnonpancreaticsecretoryPLA2sPLA2anti-inflammatoryInhibitorinhibitorinhibit

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Varespladib
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