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209006-18-8

209006-18-8 structure
209006-18-8 structure

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
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.  

Molecular Formula C59H71ClN12O8S2
Molecular Weight 1175.85
Exact Mass 1174.46000
PSA 378.11000
LogP 7.94310
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