H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 trifluoroacetate salt (Disulfide bond)

Names

[ CAS No. ]:
209006-18-8

[ Name ]:
H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 trifluoroacetate salt (Disulfide bond)

[Synonym ]:
prl-2915

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Somatostatin Receptor

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> Urotensin Receptor

[Target]

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)

[In Vitro]

PRL 2915 (0.3-30 nM; 30 min) 剂量依赖性地阻断人尿紧张素 II (human urotensin II) 诱导的大鼠主动脉环的强张性收缩[2]。

[References]

[1]. Hocart SJ, et al. Highly potent cyclic disulfide antagonists of somatostatin. J Med Chem. 1999 Jun 3;42(11):1863-71.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₉H₇₁ClN₁₂O₈S₂

[ Molecular Weight ]:
1175.85

[ Exact Mass ]:
1174.46000

[ PSA ]:
378.11000

[ LogP ]:
7.94310

Related Compounds

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