Powder: -20°C for 3 years | In solvent: -80°C for 1 year
6-Iodopravadoline (AM630) 是大麻素类CB2受体拮抗剂,其Ki=31.2 nM,选择性是 CB1 受体的 165 倍。它减弱了许多大麻素抑制小鼠离体输精管电诱发抽搐的能力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 319 | 现货 | ||
2 mg | ¥ 456 | 现货 | ||
5 mg | ¥ 651 | 现货 | ||
10 mg | ¥ 937 | 现货 | ||
25 mg | ¥ 2,130 | 现货 | ||
50 mg | ¥ 3,520 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,030 | 现货 |
产品描述 | 6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors. |
靶点活性 | CB2:(ki)31.2 nM |
体外活性 | 6-Iodopravadoline is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). 6-Iodopravadoline (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner[3]. 6-Iodopravadoline (1 μM) blocks the CP-55,940 dose response with EC50 of 170 nM at human and EC50 of 110 nM at rat cannabinoid CB2 receptor[4]. The AM251 and 6-Iodopravadoline (AM630)-evoked Ca2+?influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC50 for AM251 and 6-Iodopravadoline are 7.37 μM and 15.6 μM, respectively. AM251 and 6-Iodopravadoline activate TRPA1 in TG sensory neurons. AM251 and 6-Iodopravadoline activation of TRPA1 is modulated by TRPV1[2]. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. |
体内活性 | 6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used[1]. 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box, compared with vehicle group. |
别名 | [6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮, AM630 |
分子量 | 504.36 |
分子式 | C23H25IN2O3 |
CAS No. | 164178-33-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (99.14 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 | 1.9827 mL | 9.9136 mL | 19.8271 mL | 49.5678 mL |
5 mM | 0.3965 mL | 1.9827 mL | 3.9654 mL | 9.9136 mL | |
10 mM | 0.1983 mL | 0.9914 mL | 1.9827 mL | 4.9568 mL | |
20 mM | 0.0991 mL | 0.4957 mL | 0.9914 mL | 2.4784 mL | |
50 mM | 0.0397 mL | 0.1983 mL | 0.3965 mL | 0.9914 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。
6-Iodopravadoline 164178-33-0 GPCR/G Protein Cannabinoid Receptor Inhibitor Iodopravadoline selective AM 630 6Iodopravadoline competitive 6 Iodopravadoline AM-630 anxiolytic twitches [6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮 inhibit AM630 stimulated inhibitor