Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Linopirdine (DuP 996) 是一种口服有效的,选择性 M 型 K+电流 (IM;Kv7;KCNQ Channels) 抑制剂,IC50为 2.4 μM。Linopirdine 是TRPV1激活剂。Linopirdine 是一种公认的认知增强药物,可增加大鼠脑组织中乙酰胆碱的释放。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 313 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 777 | 现货 | ||
10 mg | ¥ 1,250 | 现货 | ||
25 mg | ¥ 2,280 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,120 | 现货 | ||
200 mg | ¥ 7,690 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 861 | 现货 |
产品描述 | Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue. |
靶点活性 | K+ current, M-type:2.4 μM |
体外活性 | Linopirdine is a well known blocker of voltage-gated potassium channels from the Kv7 (or KCNQ) family that generate the so called M current in mammalian neurons. Kv7 subunits are also expressed in pain-sensing neurons in dorsal root ganglia, in which they modulate neuronal excitability. Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1), another ion channel expressed in nociceptors and involved in pain signaling. Linopirdine induces increases in intracellular calcium concentration in human embryonic kidney 293 (HEK293) cells expressing TRPV1, but not TRPA1 and TRPM8 or in wild-type HEK293 cells. Linopirdine also activates an inward current in TRPV1-expressing HEK293 cells that is almost completely blocked by the selective TRPV1 antagonist capsazepine. At low concentrations linopirdine sensitizes both recombinant and native TRPV1 channels to heat, in a manner that is not prevented by the Kv7-channel opener flupirtine. Linopirdine exerts an excitatory action on mammalian nociceptors not only through inhibition of the M current but also through activation of the capsaicin receptor TRPV1[4]. |
体内活性 | Linopirdine (i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently enhances MAP by up to 15%[2]. |
别名 | 利诺吡啶, DuP 996 |
分子量 | 391.46 |
分子式 | C26H21N3O |
CAS No. | 105431-72-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 110 mg/mL (281 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 | 2.5545 mL | 12.7727 mL | 25.5454 mL | 63.8635 mL |
5 mM | 0.5109 mL | 2.5545 mL | 5.1091 mL | 12.7727 mL | |
10 mM | 0.2555 mL | 1.2773 mL | 2.5545 mL | 6.3863 mL | |
20 mM | 0.1277 mL | 0.6386 mL | 1.2773 mL | 3.1932 mL | |
50 mM | 0.0511 mL | 0.2555 mL | 0.5109 mL | 1.2773 mL | |
100 mM | 0.0255 mL | 0.1277 mL | 0.2555 mL | 0.6386 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。
Linopirdine 105431-72-9 Membrane transporter/Ion channel Potassium Channel TRP/TRPV Channel Kv7 enhancing DuP996 利诺吡啶 inhibit TRP Channel Inhibitor Transient receptor potential channels DuP 996 KcsA current acetylcholine DuP-996 Channels orally TRPV1 KCNQ M-type cognition inhibitor