Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is aneurokinin-1 (NK1) receptorantagonist, with anIC₅₀of 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 MDMin 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^-14M. Vapreotide inhibits GH release with an IC₅₀of 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].

1191.39

Solid

C₅₇H₇₀N₁₂O₉S₂.xC₂H₄O₂

849479-74-9

醋酸伐普肽

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : 14.29 mg/mL(11.99 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。