CAS NO: | 849479-74-9 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is aneurokinin-1 (NK1) receptorantagonist, with anIC50of 330 nM. | ||||||||||||||||
体外研究 (In Vitro) | 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]. | ||||||||||||||||
体内研究 (In Vivo) | 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 1191.39 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C57H70N12O9S2.xC2H4O2 | ||||||||||||||||
CAS 号 | 849479-74-9 | ||||||||||||||||
中文名称 | 醋酸伐普肽 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: H2O : 14.29 mg/mL(11.99 mM;Need ultrasonic) 配制储备液
* 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。 |