Varespladib

SKU: orb1225944

Description

Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3.

Key Properties

• CAS Number: 172732-68-2
• MW: 380.39
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀N₂O₅
• SMILES: NC(C(C1=C(CC)N(CC2=CC=CC=C2)C3=C1C(OCC(O)=O)=CC=C3)=O)=O
• Target: Phospholipase
• Solubility: DMSO: 76 mg/mL (199.79 mM)

Bioactivity

• In Vivo:
  Animal model: Male Hartley guinea pigs (300-500 g). 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.
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• In Vitro:
  Western blot analysis. 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 Cell line: HCjE cells. Concentration: 10 μ. Incubation time: 24 hours and 48 hours. Result: Significantly inhibited RA-induced MUC16 expression by 100% at 24 hours and 99% at 48 hours.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY315920

Quick Database Links

Gene Symbol

Phospholipase