209006-18-8

209006-18-8 structure

Name: H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 trifluoroacetate salt (Disulfide bond)
Chemical Name: H-P-CHLORO-PHE-D-CYS-β-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2
CAS Number: 209006-18-8
Molecular Formula: C₅₉H₇₁ClN₁₂O₈S₂
Molecular Weight: 1175.85
Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
Create Date: 2017-04-05 19:21:16
Modify Date: 2023-02-18 10:09:52
PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM[1].

Name	H-P-CHLORO-PHE-D-CYS-β-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2
Synonyms	prl-2915

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.