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L-745870 hydrochloride

L-745870 hydrochloride

产品编号 T11799   CAS 1173023-36-3

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。

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L-745870 hydrochloride Chemical Structure
L-745870 hydrochloride, CAS 1173023-36-3
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
其他形式的 L-745870 hydrochloride:
产品目录号及名称: L-745870 hydrochloride (T11799)
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纯度: 97.36%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

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

溶液配制表

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

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参考文献

1. Bristow LJ, et al. Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist. Trends Pharmacol Sci. 1997 Jun;18(6):186-8. 2. Patel S, et al. Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. 3. Kulagowski JJ, et al. 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem. 1996 May 10;39(10):1941-2.
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相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗帕金森病化合物库 GPCR靶点分子库 已知活性化合物库 经典已知活性库 ReFRAME 相关化合物库 抑制剂库 口服活性化合物库 神经递质受体化合物库 神经信号分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

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。

Keywords

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