化合物 LP-211|T5387|TargetMol

價(jià)格	詢價(jià)
包裝	1removed

最小起訂量	1removed
發(fā)貨地	上海
更新日期	2026-06-29

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產(chǎn)品詳情

中文名稱:化合物 LP-211	英文名稱:LP-211
CAS:1052147-86-0	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.70%	產(chǎn)品類別: 抑制劑
貨號(hào): T001\|T5387

Product Introduction

Bioactivity

名稱	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.
激酶實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	LP-211展示出高度親和5-HT 7受體（Ki = 0.58 nM），對(duì)5-HT 1A和D 2受體具有高選擇性（分別為324倍和245倍），并具有激動(dòng)劑屬性（最大效應(yīng)=82%，EC 50 = 0.60 microM）[1]。LP-211的預(yù)處理對(duì)Fos樣免疫活性無影響，但顯著增強(qiáng)了辣椒素產(chǎn)生的反應(yīng)[2]。
體內(nèi)活性	小鼠腹腔注射LP-211（10 mg/kg）后，該化合物迅速進(jìn)入全身循環(huán)并進(jìn)入大腦。其大腦濃度-時(shí)間曲線與血漿中的相似[1]。脊髓損傷（SCI）大鼠對(duì)LP-211（0.003-0.3 mg/kg, 靜脈注射）的反應(yīng)表現(xiàn)為劑量依賴性地增加膀胱容量和殘余容量[3]。LP-211降低了第5層錐體神經(jīng)元的突觸整合，這在神經(jīng)病理性疼痛中由于樹突上的超極化激活和環(huán)核苷酸調(diào)節(jié)（HCN）通道功能失調(diào)而增強(qiáng)[4]。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	10% DMSO+90% Saline : < 10 mg/mL (21.43 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (21.43 mM), Solution. DMSO : 125 mg/mL (267.88 mM), Sonication is recommended.
關(guān)鍵字	Serotonin Receptor \| LP-211 \| LP211 \| LP 211 \| Inhibitor \| inhibit \| DopamineReceptor \| Dopamine Receptor \| D2 \| 5-hydroxytryptamine Receptor \| 5HTReceptor \| 5-HT7 \| 5-HT1A \| 5-HT Receptor \| 5HT Receptor
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相關(guān)庫	血腦屏障通透化合物庫 \| 經(jīng)典已知活性庫 \| 抗癌化合物庫 \| 已知活性化合物庫 \| 神經(jīng)信號(hào)分子庫 \| 抗高血壓化合物庫 \| 抗抑郁癥化合物庫 \| GPCR靶點(diǎn)分子庫 \| 膜蛋白靶向化合物庫 \| 神經(jīng)退行性疾病化合物庫 \| 疼痛相關(guān)化合物庫 \| 共價(jià)抑制劑庫

關(guān)鍵字： LP-211;TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：14年
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