Identification | Back Directory | [Name]
[3-[[3-(2-Amino-2-oxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-5-yl]oxy]propyl]-phosphonicacid | [CAS]
164083-84-5 | [Synonyms]
LY 311727 (3-{[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid [3-[[3-(2-Amino-2-oxoethyl)-2-ethyl-1-(phenylmethyl)-1H-indol-5-yl]oxy]propyl]-phosphonicacid (3-{[3-(2-amino-2-oxoethyl)-1-benzyl-2-ethyl-1H-indol-5-yl]oxy}propyl)phosphonic acid (ApexBio) Phosphonic acid, P-[3-[[3-(2-aMino-2-oxoethyl)-2-ethyl-1-(phenylMethyl)-1H-indol-5-yl]oxy]propyl]- | [Molecular Formula]
C22H27N2O5P | [MDL Number]
MFCD00943218 | [MOL File]
164083-84-5.mol | [Molecular Weight]
430.43 |
Chemical Properties | Back Directory | [Boiling point ]
758.2±70.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥15mg/mL | [form ]
powder | [pka]
2.43±0.10(Predicted) | [color ]
white to tan |
Hazard Information | Back Directory | [Description]
Secreted phospholipase A2 (sPLA2) isoforms are low molecular weight, millimolar calcium-dependent enzymes that hydrolyze the fatty acid from the sn-2 position of membrane phospholipids. Group IIA sPLA2, also known as sPLA2IIA and non-pancreatic sPLA2, has roles in the regulation of eicosanoid synthesis and may modulate inflammatory signaling. LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 μM) that interacts with the active site of the enzyme in a non-covalent manner. It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2). LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems. | [Uses]
LY311727 is an inhibitor of Group IIA sPLA2 (IC50 = 0.47 μM) that interacts with the active site of the enzyme in a non-covalent manner. It shows greater than 1,500-fold selectivity over pancreatic sPLA2 (Group IB sPLA2). LY311727 is commonly used to distinguish the actions of Group IIA sPLA2 from those of other sPLA2 isoforms in biological systems.[Cayman Chemical]
| [Biochem/physiol Actions]
LY311727 is an orally active; potent secretory Phospholipase A2 (sPLA2; Group IIa) inhibitor. | [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: | C57BL/6J mice, 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. |
| [storage]
Store at -20°C |
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