Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC₅₀ of 330 nM.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1191.42

C₅₉H₇₄N₁₂O₁₁S₂

849479-74-9

固體

White to off-white

{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7)

{d-Phe}-CY-{d-Trp}-KVCW-NH2 (Disulfide bridge: Cys2-Cys7)

醋酸伐普肽

Room temperature in continental US; may vary elsewhere.

• [1]. Spitsin S, et al. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor. Neuroimmunomodulation. 2013;20(5):247-55.  [Content Brief]

  [2]. Hofland LJ, et al. Relative potencies of the somatostatin analogs octreotide, BIM-23014, and RC-160 on theinhibition of hormone release by cultured human endocrine tumor cells and normal rat anterior pituitary cells. Endocrinology. 1994 Jan;134(1):301-6.  [Content Brief]

  [3]. Buscail L, et al. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. Proc Natl Acad Sci U S A. 1995 Feb 28;92(5):1580-4.  [Content Brief]

  [4]. Veal N, et al. Hemodynamic effects of acute and chronic administration of vapreotide in rats with cirrhosis. Dig Dis Sci. 2003 Jan;48(1):154-61.  [Content Brief]

  [5]. Pinski J, et al. Effect of somatostatin analog RC-160 and bombesin/gastrin releasing peptide antagonist RC-3095 on growth of PC-3 human prostate-cancer xenografts in nude mice.  [Content Brief]