Vapreotide acetate|cas: 849479-74-9

Vapreotide acetate|cas: 849479-74-9

DC Chemicals, Website: www.dcchemicals.com

Product Name: Vapreotide acetate|Cas Number: 849479-74-9| Catalog Number: DC10348|Other Nmaes: RC-160 acetate; BMY-41606 acetate; RC160 acetate; BMY41606 acetate; RC 160 acetate; BMY 41606 acetate

Vapreotide acetate is a synthetic analog of somatostatin for the treatment of variceal bleeding; also exhibits antitumor activity.

Somatostatin is a peptide hormone which is distributed in many tissues including the immune system and the nervous system. Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation in a dose-dependent manner. Vapreotide also inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide inhibits HIV-1 infection of human MDM in vitro, an effect that is reversible by SP pretreatment[1]. Vapreotide significantly inhibits GH-, PRL, and/or alpha-subunit release by human GH-secreting pituitary adenoma cells in concentrations as low as 10-12-10-14 M. Vapreotide inhibits GH release with an IC50 of 0.1 pM[2]. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 (IC50=0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC50=200 and 620 nM, respectively). RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50=53 and 150 pM, respectively)[3].In cirrhosis, bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension. The acute administration of vapreotide to rats decreases collateral circulation blood flow while chronic administration attenuated its development[4]. Tumor volumes and weights are reduced by about 40% by RC-160 by s.c. injections at doses of 100 μg/day/animal. Vapreotide can inhibit the growth of androgen-independent prostate cancer when the therapy is started at an early stage of tumor development[5].