化合物 AVN-492|T5179|TargetMol

價(jià)格	￥315	￥745	￥1230
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:化合物 AVN-492	英文名稱:AVN-492
CAS:1220646-23-0	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.
純度規(guī)格: 99.29%	產(chǎn)品類別: 抑制劑
貨號(hào): T5179

Product Introduction

Bioactivity

名稱	AVN-492
描述	AVN-49 is a potent and selective 5-HT6R Antagonist (Ki: 91 pM).
激酶實(shí)驗(yàn)	Assessment of AVN-492 selectivity was performed on a panel of 69 therapeutic targets including receptors, ion channels, neuromediator transporters, and enzymes. The full list of the targets is presented in the Supplementary Material. AVN-492 interactions with therapeutic targets were assessed by either equilibrium competitive displacement of corresponding radiolabeled ligands or inhibition of corresponding enzymatic activities. The studies were performed at Eurofins in accordance with their internally optimized procedures as briefly described in. The displacement of radioligands and inhibition of enzymatic activities were measured at AVN-492 concentration of 1 M in duplicates. Affinities of AVN-492 to both the 5-HT6R and 5-HT2BR were assessed in an equilibrium competitive [3H]LSD displacement assay. AVN-492 was provided at different concentrations and [3H]LSD was kept at a concentration of 1.50 nM for 5-HT6R, or 1.20 nM for 5-HT2BR. The ligands were added to corresponding receptor-membrane suspensions (plasma membranes obtained from engineered HeLa cells expressing recombinant human 5-HT6R or engineered CHO-K1 cells expressing recombinant human 5-HT2BR). The cell membrane/ligands mixtures were incubated in buffer of the following composition: For 5-HT6R: 50 mM Tris-HCl, pH 7.4, 150 mM NaCl, 2 mM ascorbic acid, 0.001% BSA – 120 min at 37?C; for 5-HT2BR: 50 mM Tris-HCl, pH 7.4, 4 mM CaCl2, 0.1% ascorbic acid – 60 min at 37?C. Specific radio-ligand binding was measured as a difference between total binding and binding in the presence of excessive concentration of cold serotonin [1].
動(dòng)物實(shí)驗(yàn)	For pharmacokinetic, behavior, and toxicity studies, male Wistar rats (220–242 g), male CD1 mice (24–30 g), male SHK mice (20–25 g), and male Balb/C mice (15–20 g) were used. Rodents were obtained from Jackson Laboratories and housed in a standard laboratory animal facility in groups of 5–7 animals per cage. Before entering the investigation, the animals were acclimated at least for seven days. Obese C57BL/6 male 18-week-old mice were obtained from Jackson Laboratories. The mice were fed on a high-fat diet (60% kcal Research Diet 12492i) from the age of 6 weeks. Upon arrival, the mice were maintained on the same high fat diet with free access to both food and water. The mice were individually housed in solid bottom static isolators with Bed-O'Cobs? bedding inside a BioBUBBLE? clean room that provided HEPA-filtered air into the clean room environment at a rate of 100 complete air changes per hour. All treatments and procedures including body weight determinations, drug administration, and glucose measurements were carried out in the clean room environment [1].
體外活性	AVN-492與[3H]LSD競爭結(jié)合到5-HT6R的親和力估計(jì)為91 pM（IC50^b = 194 pM）。相比之下，AVN-492對(duì)5-HT2BR的親和力，Ki^b = 170 nM（IC50^b = 268 nM）。盡管AVN-492會(huì)被人類微粒體代謝，但在高達(dá)10 M濃度下，它并沒有顯著抑制五種主要的人類重組CYP同工酶，即CYP3A4、1A2、2C9、2C19和2D6 [1]。
體內(nèi)活性	AVN-492在嚙齒動(dòng)物中具有高口服生物利用度和良好的腦滲透性。在行為測(cè)試中，AVN-492在提高加迷宮模型中表現(xiàn)出抗焦慮效應(yīng)，防止了阿波嗎啡引起的驚跳起始脈沖抑制（PPI模型）的破壞，并逆轉(zhuǎn)了東莨菪堿和MK-801引起的被動(dòng)避免模型中的記憶缺損。在小鼠模型中未發(fā)現(xiàn)AVN-492具有抗肥胖效應(yīng)[1]。
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	DMSO : 7.5 mg/mL (20.87 mM), Sonication is recommended.
關(guān)鍵字	inhibit \| 5-HT Receptor \| Inhibitor \| Serotonin Receptor \| AVN 492 \| AVN-492 \| 5-hydroxytryptamine Receptor
相關(guān)產(chǎn)品	Cinchonidine \| Sevoflurane \| Cloperastine hydrochloride \| Alverine citrate \| Amitriptyline hydrochloride \| Olanzapine \| Dapoxetine hydrochloride \| Trazodone hydrochloride \| Mianserin hydrochloride \| Fluoxetine hydrochloride \| Serotonin hydrochloride \| CLOZAPINE N-OXIDE
相關(guān)庫	抑制劑庫 \| 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 \| 5-羥色胺分子庫 \| 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

關(guān)鍵字： AVN492|TargetMol

公司簡介

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 （12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
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場(chǎng)三路238號(hào)8樓

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