Vapreotide (trifluoroacetate salt) (Synonyms: BMY 41606, Octastatin, RC 160) |
| カタログ番号GC45139 |
バプレオチドは、ペプチド神経キニン-1受容体（NK1）拮抗剤であり、ソマトスタチンのアナログです（放射性リガンド結合アッセイにおけるIC50 = 330 nM）。
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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Vapreotide is a peptide neurokinin-1 receptor (NK1) antagonist and analog of somatostatin (IC50 = 330 nM in a radioligand binding assay). It inhibits increases in vascular permeability stimulated by substance P in a concentration-dependent manner in isolated guinea pig trachea and main bronchi. Vapreotide (8 nmol per animal) reduces substance P-induced biting and scratching in mice. It increases reaction time to heat stimuli in the hot plate and tail flick tests when administered at a dose of 512 μg/kg, indicating antinociceptive activity in mice. Vapreotide reduces plasma growth hormone (GH) increases induced by phenobarbital , morphine , and chlorpromazine , hypoglycemia-induced glucagon elevation, and glucose-induced insulin secretion in rats. It also decreases tumor weight and volume in a hamster model of pancreatic ductal adenocarcinoma and suppresses tumor growth and reduces GH secretion in SK-ES-1 and MNNG/HOS osteosarcoma mouse xenograft models.
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