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

Varespladib sodium (Synonyms: LY315920 sodium)

Cat. No.: HY-13402A
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Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium 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.

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Varespladib sodium Chemical Structure

Varespladib sodium Chemical Structure

CAS No. : 172733-42-5

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Description

Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium 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

sPLA2

9 nM (IC50)

In Vitro

Varespladib sodium (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 sodium (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].

Western Blot Analysis[2]

Cell Line: HCjE cells
Concentration: 10 μM
Incubation Time: 24 hours, 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, 48 hours
Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
In Vivo

Varespladib sodium 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 sodium is 16.1 mg/kg[1].

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.
Molecular Weight

402.38

Formula

C₂₁H₁₉N₂NaO₅

CAS No.

172733-42-5

SMILES

CCC1=C(C(C(N)=O)=O)C2=C(OCC(O[Na])=O)C=CC=C2N1CC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

VarespladibLY315920LY 315920LY-315920PhospholipaserecombinanthumangroupIIAnonpancreaticsecretoryPLA2sPLA2anti-inflammatoryInhibitorinhibitorinhibit

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Varespladib sodium
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