Powder: -20°C for 3 years | In solvent: -80°C for 1 year
lumateperone Tosylate (ITI-007) 是5-HT 2A 受体拮抗剂,Ki 为 0.54 nM,突触前 D2受体的部分激动剂和突触后 D2受体的拮抗剂,Ki 为 32 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 495 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,270 | 现货 | ||
100 mg | ¥ 3,400 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 622 | 现货 |
产品描述 | lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM). |
靶点活性 | SERT:61 nM (Ki), 5-HT2A receptor:0.54 nM (Ki) |
体外活性 | Lumateperone also possesses an affinity for the D1 receptor (Ki: 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki: 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold). |
别名 | ITI-007, Lumateperone甲苯磺酸盐 |
分子量 | 565.7 |
分子式 | C31H36FN3O4S |
CAS No. | 1187020-80-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 245 mg/mL (433.09 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7677 mL | 8.8386 mL | 17.6772 mL | 44.193 mL |
5 mM | 0.3535 mL | 1.7677 mL | 3.5354 mL | 8.8386 mL | |
10 mM | 0.1768 mL | 0.8839 mL | 1.7677 mL | 4.4193 mL | |
20 mM | 0.0884 mL | 0.4419 mL | 0.8839 mL | 2.2097 mL | |
50 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8839 mL | |
100 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。
lumateperone Tosylate 1187020-80-9 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor ITI-007 schizophrenia Inhibitor inhibit dopamine D1 receptor 5-HT2A 5-hydroxytryptamine Receptor ITI 007 presynaptic D2 receptor Lumateperone甲苯磺酸盐 Lumateperone ITI007 postsynaptic D2 receptor Serotonin Receptor inhibitor