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  • 化合物 L-745870|T11799L|TargetMol

化合物 L-745870|T11799L|TargetMol

L-745870
158985-00-3
￥5570 100mg 起订
￥347 2mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 L-745870
英文名称：
L-745870
CAS号：
158985-00-3
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
产品类别：
抑制剂
货号：
T11799L

Product Introduction

Bioactivity

名称L-745870
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.
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].
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
关键字L-745870 | L745870 | L 745870
相关产品Fluphenazine dihydrochloride | Octodrine | Oxolinic acid | Citicoline | Mirtazapine | Phenothiazine | Olanzapine | Mianserin hydrochloride | CLOZAPINE N-OXIDE | Doxepin hydrochloride | Octopamine hydrochloride | Promazine hydrochloride
L-745870|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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