sPLA2 inhibitor 1

Names

[ Name ]:
sPLA2 inhibitor 1

[Synonym ]:
KH064
Benzenepentanoic acid, γ-[(1-oxo-7-phenylheptyl)amino]-4-(phenylmethoxy)-, (γS)-
MFCD06411576
sPLA2 inhibitor
(4S)-5-[4-(Benzyloxy)phenyl]-4-[(7-phenylheptanoyl)amino]pentanoic acid
5-(4-Benzyloxyphenyl)-4S-(7-phenylheptanoylamino)pentanoic acid

Biological Activity

[Description]:

sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

Research Areas >> Inflammation/Immunology

[Target]

sPLA2:29 nM (IC50)

[In Vivo]

sPLA2 inhibitor 1 (compound 2b; oral; 5 mg/kg/day; on Days 10-13 after inoculation with arthritogen) shows substantial inhibition of the oedema. Drug-treated rats shows mild capsular oedema and minimal infiltration of macrophages into the red pulp[1].

[References]

[1]. Karl A Hansford, et al. D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity. Chembiochem. 2003 Mar 3;4(2-3):181-5.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
720.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₁H₃₇NO₄

[ Molecular Weight ]:
487.63

[ Flash Point ]:
389.8±32.9 °C

[ Exact Mass ]:
487.272247

[ LogP ]:
6.16

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.573

[ Storage condition ]:
2-8°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
22-24/25

[ RIDADR ]:
NONH for all modes of transport

Articles

Inhibitors of secretory phospholipase A2 group IIA.

Curr. Med. Chem. 12(25) , 3011-26, (2005)

Phospholipases A2 cleave membrane phospholipids to release arachidonic acid, the precursor to a large family of pro-inflammatory eicosanoids including prostaglandins and leukotrienes that have been pr...

Antifibrotic activity of an inhibitor of group IIA secretory phospholipase A2 in young spontaneously hypertensive rats.

J. Immunol. 176(11) , 7000-7, (2006)

The development of fibrosis in the chronically hypertensive heart is associated with infiltration of inflammatory cells and cardiac hypertrophy. In this study, an inhibitor of the proinflammatory enzy...

Group IIa secretory phospholipase expression correlates with group IIa secretory phospholipase inhibition-mediated cell death in K-ras mutant lung cancer cells.

J. Thorac. Cardiovasc. Surg. 144(6) , 1479-85, (2012)

There are currently no targeted therapies against lung tumors with oncogenic K-ras mutations that are found in 25% to -40% of lung cancers and are characterized by their resistance to epidermal growth...