keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM). 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 Vapreotide acetate 的水溶性和稳定性通常比游离态更好。
产品描述 | Vapreotide is an antagonist of the neurokinin-1 (NK1) receptor (IC50: 330 nM). |
靶点活性 | NK1R:330 nM |
体外活性 | In a concentration-dependent manner, Vapreotide attenuates the effect of SP on calcium release . The concentration required for Vapreotide to completely inhibit the effect of SP is about 100 times higher than that required for the NK1R antagonist aprepitant. The effect of Vapreotide on cell proliferation is mediated primarily by SSTR2. In order to further establish the NK1R antagonist effect of Vapreotide, U373MG cells are pretreated with SSTR2 selective antagonist CYN followed by incubation with Vapreotide and SP stimulation. The results show that pretreatment with CYN does not reverse the inhibitory effect of Vapreotide on SP-stimulated IL-8 mRNA expression. As compared to control MDM, limited HIV gag mRNA expression may indicate that Vapreotide can reduce HIV-1 replication in MDM. In addition, SP treatment (10 μM) reversed the inhibitory effect of pentoprofen on HIV-1 replication in MDM. This observation indicates that the inhibitory effect of Vapreotide on HIV-1 replication is most likely due to its interaction with NK1R. |
别名 | BMY 41606, RC160 |
分子量 | 1131.38 |
分子式 | C57H70N12O9S2 |
CAS No. | 103222-11-3 |
keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 60 mg/mL (53.03 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 0.8839 mL | 4.4194 mL | 8.8388 mL | 22.0969 mL |
5 mM | 0.1768 mL | 0.8839 mL | 1.7678 mL | 4.4194 mL | |
10 mM | 0.0884 mL | 0.4419 mL | 0.8839 mL | 2.2097 mL | |
20 mM | 0.0442 mL | 0.221 mL | 0.4419 mL | 1.1048 mL | |
50 mM | 0.0177 mL | 0.0884 mL | 0.1768 mL | 0.4419 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Vapreotide 103222-11-3 Others RC-160 BMY41606 BMY 41606 BMY-41606 RC160 RC 160 Inhibitor inhibitor inhibit