product name Varespladib (LY315920)
Description: Varespladib (aslo known as LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Varespladib reduces atherosclerosis and aneurysm formation in ApoE-/- mice and in guinea pigs. Varespladib significantly reduces the post-ACS inflammatory response in those with and without diabetes. Varespladib may be potentially useful for treatment of coronary artery disease.
References: J Med Chem. 1996 Dec 20;39(26):5159-75; J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24.
380.39
Formula
C21H20N2O5
CAS No.
172732-68-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 76 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: LY315920 exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50 of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively. In BAL cells challenged with human sPLA2, LY315920 at doses ranging from 0.1 μM–3 μM reduces the formation of thromboxane mediated by human sPLA2 in a concentration-dependent manner with an IC50 of approximately 0.8 μM. In human conjunctival epithelial cell line (HCjE), LY315920 (10 μM) significantly inhibits all-trans-retinoic acid (RA) -induced membrane-associated mucin MUC16 expression by 100% at 24 hours and 99% at 48 hours. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Ex vivo, LY315920 at doses ranging from 3 mg/kg to 30 mg/kg via i.v. inhibits human sPLA2-induced release of thromboxane from guinea pig BAL cells with ED50 of 16.1 mg/kg. In Transgenic Mice Expressing Human sPLA2, both oral and i.v. administration of LY315920 (0.3 mg/kg–3 mg/kg) abolishes serum sPLA2 activity in a dose and time dependent manner. |
| Animal model | Transgenic Mice Expressing Human sPLA2 Protein |
| Formulation & Dosage | Dissolved in 5% DMSO, 5% ethanol, and 30% polyethylene glycol 300.; ≤3 mg/kg; Oral gavage or i.v. |
| References | J Med Chem. 1996 Dec 20;39(26):5159-75; J Pharmacol Exp Ther. 1999 Mar;288(3):1117-24. |
