化合物 ARN 272|T5357|TargetMol

價(jià)格	￥125	￥197	￥347
包裝	2mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 ARN 272	英文名稱:ARN272
CAS:488793-85-7	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 98.23%	產(chǎn)品類別: 抑制劑
貨號(hào): T5357

Product Introduction

Bioactivity

名稱	ARN272
描述	ARN272 is a FAAH-like anandamide transporter (FLAT) inhibitor (IC50: 1.8 μM).
動(dòng)物實(shí)驗(yàn)	All rats were surgically implanted with intra-oral cannula under isoflurane anaesthesia. Following recovery from surgery (3 days), rats received a single adaptation trial to habituate them to the chamber and the infusion procedure. During the adaptation trial, rats were placed individually in the TR chamber and received a 2?min intra-oral infusion of water (reverse osmosis water infused at 1?mL/min). On the following day, rats received the first of two conditioning trials (separated by 72?h). On each conditioning trial, rats received a pretreatment injection of ARN272 or VEH 120?min prior to the conditioning trials. During conditioning trails, rats were intra-orally infused with a saccharin solution (0.1%) for 2?min (1?mL/min) and orofacial and somatic reactions were recorded on video. Immediately following the saccharin infusion, the rats were injected with LiCl (0.15?M) or saline, and then returned to their home cage. Two additional groups were added (after ARN272 at 3.0?mg·kg?1 attenuated gaping) where pretreatment of ARN272 at 3.0?mg·kg?1 or VEH was given 120?min prior, and with SR141716 30?min prior, to each conditioning trial. The groups were VEH-Saline (VEH-SAL), n = 9; VEH-LiCl, n = 8; 0.1?mg/kg ARN272-LiCl, n = 9; 1.0?mg/kg ARN272-LiCl, n = 8; 3.0?mg/kg ARN272-LiCl, n = 8; 1.0?mg/kg SR-3.0?mg/kg ARN272, n = 8; 1.0?mg/kg SR-VEH, n = 8. Seventy-two hours following the second conditioning trial, the rats received a drug-free TR test. During the TR test, rats were re-exposed to a 2?min intra-oral infusion of saccharin solution and their orofacial and somatic responses again recorded. All video recordings were later scored by a rater blind to the experimental conditions using ‘The Observer'. Following the TR test, the rats were returned to their home cages and at 16:00?h, their water bottles were removed to begin a water deprivation regime in preparation for the CTA test.At 08:00?h the following morning, the rats received a one-bottle test in which a graduated tube of 0.1% saccharin solution was placed on the home cage, and the amount consumed was recorded at 30 and 120?min intervals. A one-bottle test was used as there is evidence to suggest it is more sensitive in detecting between-group differences in strength of taste avoidance than a two-bottle test where both water and saccharin are made available [2].
體外活性	ARN272對(duì)FLAT的抑制似乎是選擇性的，因?yàn)檫@種化合物對(duì)幾種內(nèi)源性大麻素代謝酶幾乎沒有或沒有抑制作用。此外，ARN272對(duì)大鼠腦FAAH活性的抑制作用弱且不完全，且在與重組人FAAH-1孵育后不被顯著水解（在37°C下孵育24小時(shí)后的水解率約為5%）[1]。
體內(nèi)活性	在小鼠體內(nèi)，通過腹腔注射ARN272（1mg/kg）能夠提高血漿中阿納米酰胺（anandamide）的水平，而不影響2-AG、OEA或PEA的水平。研究指出，ARN272抑制阿納米酰胺在體外內(nèi)化和在體內(nèi)失活的效應(yīng)，以及在faah-1/ 小鼠中觀察到的阿納米酰胺積聚減少現(xiàn)象[1]。ARN272的系統(tǒng)性給藥在大鼠中產(chǎn)生了劑量依賴性地抑制因惡心引起的條件性張口行為，并在鼩鼱中減少了嘔吐的劑量依賴性降低。在大鼠中，與ARN272（3.0mg/kg）的系統(tǒng)性共同給藥能完全逆轉(zhuǎn)ARN272以1.0mg/kg抑制的張口行為。SR141716單獨(dú)使用的效果與載體溶液無差異[2]。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : Insoluble Ethanol : 8 mg/mL (18.50 mM) DMSO : 50 mg/mL (115.61 mM)
關(guān)鍵字	ARN-272 \| inhibit \| Inhibitor \| ARN272
相關(guān)產(chǎn)品	2-Chlorophenylboronic acid \| Carprofen \| MM-433593 \| JNJ-40355003 \| PF 750 \| WWL 154 \| Dual FAAH/sEH-IN-1 \| PDP-EA \| AM 374 \| VU534 \| FAAH inhibitor 1 \| Palmitoylisopropylamide
相關(guān)庫(kù)	抑制劑庫(kù) \| 脂代謝化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 代謝化合物庫(kù) \| 神經(jīng)信號(hào)分子庫(kù) \| NO PAINS 化合物庫(kù) \| 抗肥胖化合物庫(kù) \| 抗代謝疾病化合物庫(kù)

關(guān)鍵字： ARN 272|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(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)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(kù)，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。

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