Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity. 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 L-745870 trihydrochloride 的水溶性和稳定性通常比游离态更好。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 347 | 5日内发货 | ||
100 mg | ¥ 5,570 | 6-8周 |
L-745870 的其他形式现货产品:
产品描述 | L-745870 is a high-affinity and selective human dopamine D4 receptor antagonist (Ki: 0.43 nM). L-745870 has excellent brain penetration. It considerably weaker D2 (Ki: 960 nM) and D3 (Ki: 2300 nM) receptors affinity. |
靶点活性 | D2 receptor (human):960 nM(ki), D4 receptor (human):(ki)0.43 nM, D3 receptor (human):2300 nM(ki) |
体外活性 | L-745870 is an antagonist at human D4 receptors which displayed in vitro pharmacological studies. In that L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding. It blocking the inhibition of forskolin-stimulated adenylate cyclase activity in the transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells and also blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells. L-745870 inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1][2]. |
体内活性 | L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with the high brain to plasma ratios in the rat. L-745870 has no effect on apomorphine-induced stereotypy in rats but does induce catalepsy in mice, albeit at a high dose of 100 mg/kg p.o. that is likely to occupy D2 receptors in vivo. Evaluation of L-745870 in surrogate marker assays shows that this compound is freely available for biological activity in the brain and L-745870(5 to 60 mg/kg; p.o.) treatment, would occupy 50% D4 receptors in the brain. Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) causes mild sedation and extrapyramidal motor symptoms, notably bradykinesia became apparent at 30 mg/kg. High doses of L-745870 might also be expected to induce extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors. Lower doses of L-745870 has no observable behavioral effects in monkeys[1][2]. |
分子量 | 326.82 |
分子式 | C18H19ClN4 |
CAS No. | 158985-00-3 |
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。
L-745870 158985-00-3 GPCR/G Protein Neuroscience Dopamine Receptor L745870 L 745870 Inhibitor inhibitor inhibit