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Angiopeptin TFA

Names

[ CAS No. ]:
2478421-60-0

[ Name ]:
Angiopeptin TFA

Biological Activity

[Description]:

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibit adenylate cyclase or stimulate extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor
Signaling Pathways >> GPCR/G Protein >> Adenylate Cyclase

[Target]

IC50: 0.26 nM (sst2) and 6.92 nM (sst5)[1][2]


[In Vitro]

Angiopeptin (0.1 nM- 10 μM; for 1 h) TFA acts as a partial agonist (pEC50=6.57) with a maximum response of 423% at 3 μM on the release of tritium on CHO hsst2 cells[2].

[In Vivo]

Angiopeptin (20 and 50μg/kg; i.h.) TFA significantly inhibits neointimal formation[1]. Angiopeptin (20 μg/kg; per day) TFA significantly inhibits coronary artery myointimal proliferation in cardiac allografts by appmximalely 50%[1].

[References]

[1]. Lundergan CF, et al. Peptide inhibition of myointimal proliferation by angiopeptin, a somatostatin analogue. J Am Coll Cardiol. 1991;17(6 Suppl B):132B-136B.

[2]. Alderton F, et al. Somatostatin receptor-mediated arachidonic acid mobilization: evidence for partial agonism of synthetic peptides. Br J Pharmacol. 2001;132(3):760-766.

Chemical & Physical Properties

[ Molecular Formula ]:
C58H73F6N11O14S2

[ Molecular Weight ]:
1326.39


Related Compounds