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

Varespladib  (Synonyms: LY315920)

Cat. No.: HY-13402 Purity: 99.94%
COA 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

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5 mg USD 110 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 610 In-stock
100 mg USD 980 In-stock
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Based on 3 publication(s) in Google Scholar

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Varespladib Related Antibodies

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Phospholipase A PLD

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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.

Varespladib Related Antibodies

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

Appearance

Solid

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

H2O : < 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.
Purity & Documentation

Purity: 99.94%

COA (258 KB) HNMR (119 KB) RP-HPLC (167 KB) LCMS (203 KB)

Handling Instructions (2659 KB)
References
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Varespladib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

Varespladib172732-68-2LY315920LY 315920LY-315920PhospholipaseRecombinanthumangroupIIAnonpancreaticsecretoryPLA2sPLA2anti-inflammatoryInhibitorinhibitorinhibit

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