164083-84-5

164083-84-5 structure

Name: LY 311727
Chemical Name: 3-[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethylindol-5-yl]oxypropylphosphonic acid
CAS Number: 164083-84-5
Molecular Formula: C₂₂H₂₇N₂O₅P
Molecular Weight: 430.43400
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2017-06-10 14:55:27
Modify Date: 2024-01-04 09:17:15
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].

Name	3-[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethylindol-5-yl]oxypropylphosphonic acid
Synonyms	(3-{[3-(2-Amino-2-Oxoethyl)-1-Benzyl-2-Ethyl-1h-Indol-5-Yl]oxy}propyl)phosphonic Acid

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	Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase Research Areas >> Inflammation/Immunology
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.

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

RIDADR	NONH for all modes of transport

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