Vapreotide acetate 是神经激肽-1 (NK1) 受体拮抗剂，IC50值为 330 nM。

Vapreotide acetate is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM).

In a dose-dependent manner, Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation.in HEK293-NK1R and U373MG cell lines, Vapreotide inhibits SP-induced IL-8 and MCP-1 production. In vitro, Vapreotide inhibits HIV-1 infection of human MDM, 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 (IC50: 0.1 pM) [2]. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 with IC50 of 0.17, 0.1, and 21 nM, respectively, and low affinity for SSTR1 and -4 with IC50 of 200 and 620 nM, respectively. RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC50s: 53 and 150 pM) [3].

Bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension in cirrhosis. 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. When the therapy is started at an early stage of tumor development Vapreotide can inhibit the growth of androgen-independent prostate cancer [5].

849479-74-9

C59H74N12O11S2

1191.42

BMY-41606 acetate;醋酸伐普肽;RC-160 acetate

H2O:14 mg/mL (11.75 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years