Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB-616234-A 是选择性的,口服有效的5-HT1B receptor 拮抗剂。SB-616234-A 具有抗焦虑和抗抑郁活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,120 | 现货 | ||
5 mg | ¥ 5,180 | 现货 | ||
10 mg | ¥ 7,330 | 现货 | ||
25 mg | ¥ 10,800 | 现货 | ||
50 mg | ¥ 14,600 | 现货 | ||
100 mg | ¥ 19,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 6,810 | 现货 |
产品描述 | SB-616234-A is a selective and orally bioavailable antagonist of 5-HT1B receptor, with anxiolytic and antidepressant activity. |
体外活性 | SB-616234A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2). Similarly, rat and guinea pig striatal 5-HT1B receptors affinity (pKi) of 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively)[2]. |
体内活性 | SB-616234A reverses the agonist of 5-HT1/7 receptor, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively[1].a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors caused by SB-616234A (0.3-30 mg/kg p.o.) with an ED50 of 2.83 ± 0.39 mg/kg p.o[1]. |
别名 | SB-616234A |
分子量 | 574.11 |
分子式 | C32H36ClN5O3 |
CAS No. | 908601-49-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.79 mg/ml (10.08 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7418 mL | 8.7091 mL | 17.4183 mL | 43.5457 mL |
5 mM | 0.3484 mL | 1.7418 mL | 3.4837 mL | 8.7091 mL | |
10 mM | 0.1742 mL | 0.8709 mL | 1.7418 mL | 4.3546 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。
SB-616234-A 908601-49-0 GPCR/G Protein Neuroscience 5-HT Receptor inhibit 5-hydroxytryptamine Receptor SB 616234 A Inhibitor SB-616234A Serotonin Receptor SB616234A inhibitor