化合物 RS-127445|T6973|TargetMol

價(jià)格	￥189	￥423	￥677
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 RS-127445	英文名稱:RS-127445
CAS:199864-87-4	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: 98.81%	產(chǎn)品類別: 抑制劑
貨號(hào): T6973

Product Introduction

Bioactivity

名稱	RS-127445
描述	RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
細(xì)胞實(shí)驗(yàn)	RS-127445, vehicle or other antagonists are pre-incubated with 240 μl of HEK-293 cells expressing the human 5-HT2B receptor suspension at 37 °C for 20 min. HEK-293 cells are incubated with[3H]-myoinositol (1.67 μCi/ml) in 162 cm2 flasks overnight at 37 °C in an inositol free Ham's F12 medium containing 10% dialyzed foetal bovine serum. The cells are harvested, washed five times with phosphate bufffered saline and resuspended in inositol free Ham's F12 media at density of approximately 3×103 cells/ml. The reactions are initiated by addition of 5-HT. Sixty minutes later, the reactions are terminated by adding 50 μl of ice-cold 20% perchloric acid, chilled in an ice-water bath for 10 min and then neutralized with 160μl of 1 N KOH. Each sample is diluted with 2 ml of 50 mM Tris-HCl, pH 7.4 at room temperature. The aqueous portion (2.2 ml) is transferred onto Dowex AG1X8 columns (1 ml, 1 : 1, w/v) which has been washed with 5 ml of distilled water. The columns are then washed with 18 ml of distilled water and the inositol phosphates are eluted with 3 ml of 1 N HCl. The eluted radioactivity is determined by liquid scintillation spectroscopy using a Packard 1900CA analyzer. [1] (Only for Reference)
激酶實(shí)驗(yàn)	Radioligand binding: The selectivity of RS-127445 for 5-HT2B receptors is examined by testing the compound for affinity at over 100 additional ion channel or receptor binding sites. CHO-K1 cells expressing human 5-HT2A, 5-HT2B or 5-HT2C receptors are harvested using 2 mM EDTA in phosphate buffered saline. Cell membranes are prepared by four cycles of homogenization and centrifugation (48,000×g for 15 min). Each assay is established so as to achieve steady state conditions and to optimize specific binding. For the 5-HT2A receptor, membranes from 1×106 cells are incubated with 0.2 nM [3 H]-ketanserin at 32 °C for 60 min. Nonspecific binding is determined using 10 μM methysergide. For the 5-HT2B receptor, membranes from 1.5×106 cells are incubated with 0.2 nM [3 H]-5-HT at 48 °C for 120 min. Nonspecific binding is determined using 10 μM 5-HT. For the 5-HT2Creceptor, membranes from 3×10 5 cells are incubated with 0.5 nM [3 H]-mesuler -gine at 32 °C for 60 min. Nonspecific binding is determined using 10 μM methysergide. Assays are terminated by vacuum filtration through glass fibre filters(GF/B) which has been pretreated with 0.1% polyethyleneimine. Total and bound radioactivity is determined by liquid scintillation counting. Greater than 90% specific binding is achieved in each of these assays.
體外活性	RS-127445是一種新型高親和力、選擇性5-HT2B受體拮抗劑，沒有可檢測(cè)的固有活性。RS-127445對(duì)5-HT2B受體的親和力達(dá)到nM級(jí)別，具有1000倍的選擇性。RS-127445能強(qiáng)效阻斷5-HT引起的肌醇磷酸生成增加，并以比約漢賓高1000倍的效能阻斷5-HT引起的細(xì)胞內(nèi)鈣濃度增加。[1]
體內(nèi)活性	RS-127445經(jīng)口服和腹膜內(nèi)給藥后迅速吸收，不受劑量或給藥方式限制，血漿濃度在給藥后15分鐘內(nèi)達(dá)到峰值。血漿中RS-127445的濃度與給藥劑量成正比。5 mg/kg劑量下，RS-127445的生物利用度約為腹膜內(nèi)給藥的60%和口服的14%。預(yù)計(jì)，RS-127445在血漿中的濃度足以完全飽和大鼠可接觸的5-HT2B受體，并可維持該狀態(tài)。口服1到10 mg/kg的RS-127445能顯著抑制由束縛應(yīng)激引起的內(nèi)臟過敏性，抑制率達(dá)35%至74%。口服RS-127445能顯著抑制TNBS誘導(dǎo)的內(nèi)臟過敏性（3到30 mg/kg時(shí)的抑制率為15%到62%）?？诜?到30 mg/kg的RS-127445還能劑量依賴性地減少原生及TNBS處理的大鼠由束縛應(yīng)激引起的排便。[2]。RS-127445抑制結(jié)腸運(yùn)動(dòng)和排便。[3]
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	Ethanol : 8 mg/mL (28.43 mM) DMSO : 52 mg/mL (184.8 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
關(guān)鍵字	RS-127445 \| MT 500 \| inhibit \| Inhibitor \| MT-500 \| Serotonin Receptor \| 5-HT Receptor \| RS127445 \| RS 127445 \| 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(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 神經(jīng)遞質(zhì)受體化合物庫(kù) \| 高選擇性抑制劑庫(kù) \| 臨床前化合物庫(kù) \| GPCR靶點(diǎn)分子庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 神經(jīng)退行性疾病化合物庫(kù) \| 疼痛相關(guān)化合物庫(kù)

關(guān)鍵字： MT500|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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