| Bioactivity | 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]. | ||||||||||||
| Target | sPLA2 | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | LY-311727 | ||||||||||||
| CAS | 164083-84-5 | ||||||||||||
| Formula | C22H27N2O5P | ||||||||||||
| Molar Mass | 430.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. [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 |