化合物 LP-211|T5387|TargetMol

LP-211
1052147-86-0

￥283 1mg 起订

￥395 2mg 起订

￥652 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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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 LP-211

英文名称：: LP-211

CAS号：: 1052147-86-0

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.

纯度规格：: 98.65%

产品类别：: 抑制剂

货号：: T5387

Product Introduction

Bioactivity

名称	LP-211
描述	LP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor.
激酶实验	Human 5-HT1A serotonin receptors stably expressed in HEK293 cells were radiolabeled with 1.0 nM [3H]-8-OH-DPAT. Samples containing 40 μg of membrane protein and different concentrations of each compound ranging from 0.1 nM to 10 μM were incubated in a final volume of 500 μL of 50 mM Tris-HCl pH 7.4, 5 mM MgSO4 for 120 min at 37 °C. After this incubation time, samples were filtered through GF/C presoaked in polyethylenimine 0.5% for at least 30 min prior to use. The filters were washed twice with 1 mL of ice-cold buffer (50 mM Tris-HCl, pH 7.4). Nonspecific binding was determined in the presence of 10 μM 5-HT [1].
动物实验	Mice were given the test compounds intraperitoneally (10 mg/kg) and were killed by decapitation at various times thereafter. Mixed arteriovenous trunk blood was collected in heparinized tubes, centrifuged at 3000g for 10 min, and the plasma was stored at -20 °C. Brain was removed immediately, blotted with paper to remove surface blood, and quickly frozen in dry ice. Compounds and their 1-arylpiperazine metabolites were extracted from plasma and brain homogenate and quantified by reversed-phase HPLC with UV detection (230 nm). Briefly: to 0.1 mL of plasma, 0.2 mL of 20 mM of ammonium bicarbonate and 0.02 mL of a methanolic solution of the internal standard (100 μg/mL) were added; samples were then extracted twice with 1.5 mL of hexane containing 1% of isoamyl alcohol, and the combined extracts were evaporated to dryness and reconstituted in 0.15 mL of the mobile phase, which was injected into the chromatographic column. Brain tissue was homogenized in distilled water (1 g/10 mL), and 1 mL of the homogenate was extracted twice with 1.5 mL of hexane/isoamyl alcohol as described for plasma. Then, the organic phase was shaken with 0.2 mL of the mobile phase (LP-211 only); after centrifugation, 0.1 mL of the aqueous phase was injected into the chromatographic column [1].
体外活性	LP-211展示出高度亲和5-HT 7受体（Ki = 0.58 nM），对5-HT 1A和D 2受体具有高选择性（分别为324倍和245倍），并具有激动剂属性（最大效应=82%，EC 50 = 0.60 microM）[1]。LP-211的预处理对Fos样免疫活性无影响，但显著增强了辣椒素产生的反应[2]。
体内活性	小鼠腹腔注射LP-211（10 mg/kg）后，该化合物迅速进入全身循环并进入大脑。其大脑浓度-时间曲线与血浆中的相似[1]。脊髓损伤（SCI）大鼠对LP-211（0.003-0.3 mg/kg, 静脉注射）的反应表现为剂量依赖性地增加膀胱容量和残余容量[3]。LP-211降低了第5层锥体神经元的突触整合，这在神经病理性疼痛中由于树突上的超极化激活和环核苷酸调节（HCN）通道功能失调而增强[4]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 90 mg/mL (192.87 mM)
关键字	Inhibitor \| 5-HT Receptor \| LP211 \| Serotonin Receptor \| 5-hydroxytryptamine Receptor \| inhibit \| LP 211 \| LP-211
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相关库	血管生成库 \| 经典已知活性库 \| 已知活性化合物库 \| 神经递质受体化合物库 \| 神经信号分子库 \| NO PAINS 化合物库 \| GPCR靶点分子库 \| 膜蛋白靶向化合物库 \| 神经退行性疾病化合物库 \| 疼痛相关化合物库

LP-211|TargetMol

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。

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