Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AT-121 是一种双重μ-阿片和神经肽受体部分激动剂(Kis 分别为 16.49 和 3.67 nM)。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合(EC50s 分别为 19.6 和 34.7 nM)。AT-121(0.003-0.03 mg/kg)能以剂量依赖的方式降低辣椒素诱导的热异感,但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中,AT-121 每次注射剂量为 0.3 至 10 μg/kg,它缺乏强化作用(一种潜在的滥用标志),不能减少食物颗粒的强化作用。AT-121(0.01 或 0.03 毫克/千克)不会诱发恒河猴的超痛觉,超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药,具有抗伤害和止痛作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,350 | 现货 | ||
5 mg | ¥ 5,630 | 现货 | ||
10 mg | ¥ 7,790 | 现货 | ||
25 mg | ¥ 11,200 | 现货 | ||
50 mg | ¥ 13,800 | 现货 | ||
100 mg | ¥ 17,500 | 现货 | ||
500 mg | ¥ 34,800 | 现货 |
产品描述 | AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects. |
靶点活性 | Nociception:3.67 nM(Ki ), μ opioid receptor:16.49 nM(Ki ), [35S]-GTPγS:19.6 nM(EC50), [35S]-GTPγS:34.7 nM(EC50) |
体内活性 |
AT-121 (0.003-0.03 mg/kg; s.c.; rhesus monkeys) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner.[1]
AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys.[1] |
分子量 | 462.65 |
分子式 | C24H38N4O3S |
CAS No. | 2099681-31-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (118.88 mM)
Chloroform: 9.0 mg/mL (19.4 mM)
DMF: Miscible
Ethanol: Miscible
Ethanol:PBS (pH 7.2) (1:20): 50 μg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Chloroform | 1 mM | 2.1615 mL | 10.8073 mL | 21.6146 mL | 54.0365 mL |
5 mM | 0.4323 mL | 2.1615 mL | 4.3229 mL | 10.8073 mL | |
10 mM | 0.2161 mL | 1.0807 mL | 2.1615 mL | 5.4037 mL | |
DMSO | 20 mM | 0.1081 mL | 0.5404 mL | 1.0807 mL | 2.7018 mL |
50 mM | 0.0432 mL | 0.2161 mL | 0.4323 mL | 1.0807 mL | |
100 mM | 0.0216 mL | 0.1081 mL | 0.2161 mL | 0.5404 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。
AT-121 2099681-31-7 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor AT121 AT 121 Inhibitor inhibitor inhibit