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

Names

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

[Synonym ]:
H-p-Chloro-Phe-D-Cys-b-(3-pyridyl)-Ala-D-Trp-N-Me-Lys-Thr-Cys-2-Nal-NH2

Biological Activity

[Description]:

PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively)[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

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

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

[Target]

hsst5:6 nM (Ki)

hsst2:17 nM (Ki)

hsst3:66 nM (Ki)

hsst1:1000 nM (Ki)

hsst4:1000 nM (Ki)

rat urotensin II receptor:429 nM (Ki)

human urotensin II receptor:1846 nM (Ki)

[In Vitro]

PRL 3195 抑制人尿紧素 II (human urotensin II) 诱导的大鼠主动脉相位振荡，ED50 为 24 nM[1]。

[References]

[1]. 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 ]:
C₅₈H₇₁ClN₁₂O₉S₂

[ Molecular Weight ]:
1179.84000

[ Exact Mass ]:
1178.46000

[ PSA ]:
416.55000

[ LogP ]:
6.00420

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.