849479-74-9
中文名称 | 849479-74-9 |
---|---|
中文同义词 | RC-160 ACETATE; BMY-41606 ACETATE |
英文名称 | VAPREOTIDE ACETATE |
英文同义词 | VAPREOTIDE ACETATE;Vapreotide (RC160) acetate;Vapreotide acetate (1:x);BMY 41606 acetate;BMY41606 acetate;BMY-41606 acetate;RC 160 acetate;RC160 acetate |
CAS号 | 849479-74-9 |
分子式 | C59H74N12O11S2 |
分子量 | 1191.43 |
EINECS号 | |
相关类别 | 多肽中间体 |
Mol文件 | 849479-74-9.mol |
结构式 |
849479-74-9 性质
熔点 | 176-180°C |
---|---|
储存条件 | Hygroscopic, Refrigerator, under inert atmosphere |
溶解度 | 可溶于醋酸(少许)、甲醇(少许) |
形态 | 固体 |
颜色 | 白色至类白色 |
稳定性 | 吸湿性 |
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. 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 IC 50 of 0.1 pM. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 (IC 50 =0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC 50 =200 and 620 nM, respectively). RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC 50 =53 and 150 pM, respectively).
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. 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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-P0061A | 849479-74-9 Vapreotide acetate | 849479-74-9 | 5mg | 800元 |
2024/04/30 | HY-P0061A | 849479-74-9 Vapreotide acetate | 849479-74-9 | 10mg | 1300元 |