H-P-CHLORO-PHE-D-CYS-BETA-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2 Chemical Properties

Boiling point:

1507.0±65.0 °C(Predicted)

Density 

1.38±0.1 g/cm3(Predicted)

pka

12.65±0.70(Predicted)

form 

Solid

color 

White to off-white

Sequence

{Phe<4-Cl>}-{d-Cys}-{β-Ala<3-Py>}-{d-Trp}-Lys-{Val<3-Me>}-Cys-{2-Nal}-NH2(Disulfide bond)

H-P-CHLORO-PHE-D-CYS-BETA-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2 Usage And Synthesis

Uses

PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM[1].

IC 50

hsst₂: 12 nM (Ki); hsst₃: 100 nM (Ki); hsst₅: 520 nM (Ki); hsst₄: 895 nM (Ki); hsst₁: >1000 nM (Ki); hsst₂: 1.8 nM (IC₅₀, rat antagonist bioassay versus somatostatin); rat urotensin II receptor: 293 nM (Ki); human urotensin II receptor: 562 nM (Ki)

References

[1] Hocart SJ, et al. Highly potent cyclic disulfide antagonists of somatostatin. J Med Chem. 1999 Jun 3;42(11):1863-71. DOI:10.1021/jm9806289
[2] Rossowski WJ, et al. Human urotensin II-induced aorta ring contractions are mediated by protein kinase C, tyrosine kinases and Rho-kinase: inhibition by somatostatin receptor antagonists. Eur J Pharmacol. 2002 Mar 8;438(3):159-70. DOI:10.1016/s0014-2999(02)01341-9

H-P-CHLORO-PHE-D-CYS-BETA-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2(209006-18-8)Related Product Information

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