LY 311727

Modify Date: 2024-01-04 09:17:15

LY 311727 Structure
LY 311727 structure
Common Name LY 311727
CAS Number 164083-84-5 Molecular Weight 430.43400
Density 1.32g/cm3 Boiling Point 758.2ºC at 760mmHg
Molecular Formula C22H27N2O5P Melting Point N/A
MSDS N/A Flash Point 412.3ºC

 Use of 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].

 Names

Name 3-[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethylindol-5-yl]oxypropylphosphonic acid
Synonym More Synonyms

 LY 311727 Biological Activity

Description 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].
Related Catalog
Target

sPLA2[1]

In Vitro 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 1μM, 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 Mt-sPLA2 transgenic the intravenous (i.v.) administration[2]. Animal Model: C57BL/6J mice, metallothionein promoter-human secretory PLA2 minigene (Mt-sPLA2) transgenic mice model[2] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Intravenous injection Result: Significantly and dose dependently suppressed the PLA2 activity in the serum.
References

[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 Chem. 1998 Jun 5;273(23):14411-23.

 Chemical & Physical Properties

Density 1.32g/cm3
Boiling Point 758.2ºC at 760mmHg
Molecular Formula C22H27N2O5P
Molecular Weight 430.43400
Flash Point 412.3ºC
Exact Mass 430.16600
PSA 125.58000
LogP 4.37610
Vapour Pressure 3.69E-24mmHg at 25°C
Index of Refraction 1.619
Storage condition 2-8°C

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

(3-{[3-(2-Amino-2-Oxoethyl)-1-Benzyl-2-Ethyl-1h-Indol-5-Yl]oxy}propyl)phosphonic Acid
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