Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-745870 hydrochloride 是可透过血脑屏障的、选择性的、具有口服活性的多巴胺 D4受体拮抗剂,Ki=0.43 nM。它对 D2(Ki 为 960 nM) 和 D3(Ki 为 2300 nM) 受体的亲和力相对较弱,对 5-HT2受体,sigma 位点和 α-肾上腺素受体表现出中等亲和力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
2 mg | ¥ 392 | 现货 | ||
5 mg | ¥ 519 | 现货 | ||
10 mg | ¥ 893 | 现货 | ||
25 mg | ¥ 1,690 | 现货 | ||
50 mg | ¥ 2,830 | 现货 | ||
100 mg | ¥ 3,970 | 现货 | ||
500 mg | ¥ 8,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 543 | 现货 |
产品描述 | L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM. |
靶点活性 | Human dopamine D2 receptor:960 nM(Ki), Human dopamine D4 receptor:0.43 nM(Ki), Human dopamine D3 receptor:2300 nM(Ki) |
体外活性 | In vitro pharmacological studies revealed that L-745870 is an antagonist at human D4 receptors, in that L-745870 antagonized the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding,?blocked the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells,?blocked dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells,?inhibited D4 activation of cloned G protein-coupled inwardly rectifying K+ channels,?and antagonized dopamine-induced stimulation of extracellular acidification in transfected cells[1]. |
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 high brain to plasma ratios in rat[1].?Evaluation of L-745870 in surrogate marker assays demonstrates that this compound is freely available for biological activity in the brain and that at doses of 5 to 60 mg/kg p.o. L-745870 would occupy 50% D4 receptors in the brain.?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.?High doses of L-745870 might also be expected to cause extrapyramidal symptoms in primates because the levels in the CNS at these doses would be sufficient to antagonize D2 receptors.?Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg[1]. |
分子量 | 363.28 |
分子式 | C18H20Cl2N4 |
CAS No. | 1173023-36-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (137.63 mM), sonification is recommended.
0.1 M HCL: 20 mg/mL (55.05 Mm), Need ultrasonic and adjust pH to 3 with HCl
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7527 mL | 13.7635 mL | 27.527 mL | 68.8174 mL |
5 mM | 0.5505 mL | 2.7527 mL | 5.5054 mL | 13.7635 mL | |
10 mM | 0.2753 mL | 1.3763 mL | 2.7527 mL | 6.8817 mL | |
20 mM | 0.1376 mL | 0.6882 mL | 1.3763 mL | 3.4409 mL | |
50 mM | 0.0551 mL | 0.2753 mL | 0.5505 mL | 1.3763 mL | |
100 mM | 0.0275 mL | 0.1376 mL | 0.2753 mL | 0.6882 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。
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