LY-311727 

LY-311727 is a potent secretory non-pancreatic phospholipase A₂ (sPLA₂) inhibitor (IC₅₀ <1 μM for group IIA sPLA₂). sPLA₂ is an important proinflammatory enzyme^[1][2].

sPLA₂^[1]

LY-311727 (0.1-10 μM) suppresses the contractile responses induced by human non-pancreatic secretory phospholipase A₂ (hnps-PLA₂), in a concentration related manner^[1].
LY-311727 nearly abolishes the hnps-PLA₂ responses at 1 μM, while it failed to suppress porcine pancreatic PLA₂ concentration response curves at the same concentration^[1].
LY-311727 displays 1,500-fold selectivity when assayed against porcine pancreatic s-PLA₂^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LY-311727 (3-30 mg/kg; i.v.) dramatically suppresses the circulating enzyme activity in mice with metallothionein promoter-human secretory PLA₂ minigene (Mt-sPLA₂) transgenic the intravenous (i.v.) administration^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

430.43

C₂₂H₂₇N₂O₅P

164083-84-5

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. R W Schevitz, et al. Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2. Nat Struct Biol. 1995 Jun;2(6):458-65.  [Content Brief]

  [2]. N Fox, et al. Transgenic model for the discovery of novel human secretory non-pancreatic phospholipase A2 inhibitors. Eur J Pharmacol. 1996 Jul 18;308(2):195-203.  [Content Brief]

  [3]. M Murakami, et al. The functions of five distinct mammalian phospholipase A2S in regulating arachidonic acid release. Type IIa and type V secretory phospholipase A2S are functionally redundant and act in concert with cytosolic phospholipase A2. J Biol Che  [Content Brief]