Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cells. Meclinertant has anxiolytic, anti-addictive, and memory-impairing effects.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 560 | 现货 | ||
5 mg | ¥ 2,130 | 现货 | ||
10 mg | ¥ 3,940 | 现货 |
产品描述 | Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cells. Meclinertant has anxiolytic, anti-addictive, and memory-impairing effects. |
体外活性 | Meclinertant displaces 125I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8 nM for adult mouse brain and 82.0 nM for adult rat brain). Meclinertant competitively inhibits 125I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC50 values of 0.99 nM (guinea pig), 4.0 nM (rat mesencephalic cells), 7.6 nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7 nM (newborn mouse brain), 17.8 nM (newborn human brain), 8.7 nM (adult human brain), and 30.3 nM (HT-29 cells). Meclinertant blocks K+-evoked release of [3H]dopamine stimulated by neurotensin with a potency (IC50 = 0.46 nM) that correlates with its binding affinity, in guinea pig striatal slices[1]. |
体内活性 | Meclinertant (80 μg/kg; in mice) treatment, reverses the turning behavior caused by the intrastriatal injection of neurotensin. It also has a long duration of action (6 hours)[1]. |
别名 | SR 48692 |
分子量 | 587.07 |
分子式 | C32H31ClN4O5 |
CAS No. | 146362-70-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Meclinertant 146362-70-1 Others SR-48692 SR48692 SR 48692 Inhibitor inhibitor inhibit