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 | 2024-12-12 |
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: T5179 |
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5-HT2BR的親和力,Ki^b = 170 nM(IC50^b = 268 nM)。盡管AVN-492會被人類微粒體代謝,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在嚙齒動物中具有高口服生物利用度和良好的腦滲透性。在行為測試中,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 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 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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