| Description | Vapreotide acetate (BMY-41606 acetate) is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM). |
| In vitro | 按剂量依赖性，Vapreotide减弱了SP（物质P）引发的HEK293-NK1R和U373MG细胞系内的细胞内钙增加和NF-κB激活。Vapreotide抑制SP诱导的IL-8和MCP-1的产生。体外试验中，Vapreotide能够抑制人MDM的HIV-1感染，此作用通过SP预处理可逆转[1]。Vapreotide在低至10(-12)-10(-14) M的浓度下显著抑制人垂体腺瘤细胞释放GH、PRL和/或α亚单位。Vapreotide抑制GH释放（IC50：0.1 pM）[2]。Vapreotide对SSTR2、-3和-5表现出中等至高亲和力，IC50分别为0.17、0.1和21 nM，而对SSTR1和-4的亲和力较低，IC50分别为200和620 nM。RC-160抑制表达SSTR2和SSTR5的CHO细胞的血清诱导增殖（EC50s：53 和 150 pM）[3]。 |
| In vivo | 食管胃静脉曲张破裂出血是肝硬化门脉高压的严重并发症。急性给药实验中，Vapreotide降低大鼠侧支循环的血流量，而长期给药则减缓了其发展[4]。RC-160通过皮下注射，每日每只动物100 μg剂量，可减少肿瘤体积和重量约40%。若在肿瘤发展早期开始治疗，Vapreotide能够抑制雄激素非依赖性前列腺癌的增长[5]。 |
| Target activity | NK1:330 nM |
| Synonyms | RC-160 acetate, 醋酸伐普肽, BMY-41606 acetate |
| molecular weight | 1191.42 |
| Molecular formula | C59H74N12O11S2 |
| CAS | 849479-74-9 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 14 mg/mL (11.75 mM), Sonication is recommended. |
| References | 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. 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. 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. 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. 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. |