Bioactivity | Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2). |
Target | phospholipase A2 (PLA2) |
Invitro | Varespladib methyl (LY333013) is an orally-administered methyl ester pro-drug that is metabolized to LY315920[1]. Varespladib and its orally bioavailable prodrug, Varespladib methyl (methyl-Varespladib) shows high-level secretory PLA2 (sPLA2) inhibition at nanomolar and picomolar concentrations against 28 medically important snake venoms from six continents[2]. |
Name | Varespladib methyl |
CAS | 172733-08-3 |
Formula | C22H22N2O5 |
Molar Mass | 394.42 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Reference | [1]. Bradley JD, et al. A randomized, double-blinded, placebo-controlled clinical trial of LY333013, a selective inhibitor of group II secretory phospholipase A2, in the treatment of rheumatoid arthritis. J Rheumatol. 2005 Mar;32(3):417-23. [2]. Lewin M, et al. Varespladib (LY315920) Appears to Be a Potent, Broad-Spectrum, Inhibitor of Snake Venom Phospholipase A2 and a Possible Pre-Referral Treatment for Envenomation. Toxins (Basel). 2016 Aug 25;8(9). pii: E248. |