Identification | Back Directory | [Name]
H-P-CHLORO-PHE-D-CYS-BETA-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2 | [CAS]
209006-18-8 | [Synonyms]
PRL-2915 H-Phe(4-Cl)-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 H-P-CHLORO-PHE-D-CYS-β-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2 H-p-Chloro-Phe-D-Cys-b-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 H-P-CHLORO-PHE-D-CYS-BETA-(3-PYRIDYL)-ALA-D-TRP-LYS-TBU-GLY-CYS-2-NAL-NH2 H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 (Disulfide bond) H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 (Disulfide bond) {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, (DISULFIDE BOND) H-p-Chloro-Phe-D-Cys-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2((Disulfide bridge:DCys2-Cys7)) H-p-Chloro-Phe-D-Cys-b-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2 trifluoroacetate salt (Disulfide bond) H-p-Chloro-Phe-D-Cys-β-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH? trifluoroacetate salt (Disulfide bond) L-Alaninamide, 4-chloro-L-phenylalanyl-D-cysteinyl-3-(3-pyridinyl)-L-alanyl-D-tryptophyl-L-lysyl-3-methyl-L-valyl-L-cysteinyl-3-(2-naphthalenyl)-, cyclic (2→7)-disulfide | [Molecular Formula]
C59H71ClN12O8S2 | [MDL Number]
MFCD08704656 | [MOL File]
209006-18-8.mol | [Molecular Weight]
1175.85 |
Chemical Properties | Back Directory | [Boiling point ]
1507.0±65.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.65±0.70(Predicted) | [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) |
Hazard Information | Back Directory | [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 |
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