化合物 NPS 2143|T1730|TargetMol

價格	￥228	￥497	￥729
包裝	1mg	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 NPS 2143	英文名稱:NPS-2143
CAS:284035-33-2	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: 98.24%	產(chǎn)品類別: 抑制劑
貨號: T1730

Product Introduction

Bioactivity

Name	NPS-2143
Description	NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.
Kinase Assay	This clonal cell line, referred to as HEK 293 4.0-7 cells, are used in a high-throughput screening format to detect agonists and allosteric activators of the Ca2+?receptor. Changes in the concentration of cytoplasmic [Ca2+]i provide a quantitative and functional assessment of Ca2+ receptor activity in these cells and the results using this assay parallel those obtained using a homologous expression system of bovine parathyroid cells. On-line continuous measurements of fluorescence in fluo-3- or fura-2-loaded HEK 293 4.0-7 cells are obtained using a custom-built spectrofluorimeter or a fluorescence imaging plate reader instrument. NPS-2143 is incubated with cells for 1 minute before increasing the concentration of extracellular Ca2+?from 1.0 mM to 1.75 mM. NPS-2143 is tested individually at a concentration of 100 μg/mL (20 μM-80 μM) and those causing more than a 40% inhibition of the control response are considered to be biologically active. To determine the potencies (IC50) of NPS-2143 with biological activity, concentration-response curves are obtained and then, as an initial assessment of selectivity, the effects of NPS-2143 on [Ca2+]i evoked by other G protein-coupled receptors are examined at a concentration several times their IC50. Wild-type HEK 293 cells (and HEK 293 4.0-7 cells) express receptors for thrombin, bradykinin, and ATP, which couple to the mobilization of intracellular Ca2+. These responses can be studied to quickly assess any nonselective action of compounds on G protein-coupled receptors. Additional assays for selectivity include HEK 293 cells engineered to express receptors most homologous in sequence and topology to the Ca2+ receptor. These include native or chimeric receptors for various metabotropic glutamate and γ-aminobutyric acid type B receptors (GABABRs).Chimeric receptors are created using partial sequences of metabotropic glutamate receptors and Ca2+?receptors, engineered to couple to activation of phospholipase C and release of intracellular Ca2+?in HEK 293 cells. NPS-2143 lacking pan-activity are then subjected to structural modifications and their potencies and selectivities monitored using these HEK 293 4.0-7 cell assays in an iterative process.
In vitro	NPS 2143刺激牛甲狀旁腺細胞分泌甲狀旁腺激素（PTH）,EC50 為41 nM。此外,NPS 2143會阻斷擬鈣劑NPS R-467對PTH從牛甲狀旁腺細胞分泌的抑制作用以及細胞外Ca2+對異丙腎上腺素刺激的環(huán)AMP形成增加的抑制作用。表達人Ca2+受體的HEK 293細胞中,NPS 2143阻斷Ca2+受體激活誘發(fā)的細胞質(zhì)Ca2+濃度增加,IC50為43 nM。在短暫表達hCaSRs的HEK-293細胞中,NPS 2143通過有效抑制GSH (數(shù)據(jù)未顯示)和γ-Glu-Val-Gly活性,明顯抑制厚味味覺。
In vivo	在血壓正常的大鼠體內(nèi),靜脈注射NPS 2143（1 mg/kg）在甲狀旁腺存在的情況下顯著增加平均動脈血壓（MAP）.在大鼠體內(nèi),NPS 2143導致血漿PTH水平迅速增加4-5倍,并且血漿Ca 2+水平也瞬時升高.
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : ＜1 mg/mL (2.45 mM）, Sonication is recommended.
Keywords	SB-262470A \| Inhibitor \| inhibit \| Calcium-sensing receptor \| SB 262470 \| CaSR \| NPS-2143 \| NPS2143 \| SB-262470
Inhibitors Related	Nisoldipine \| 1-Octanol \| 2,5-Di-tert-butylhydroquinone \| Strontium chloride \| Levetiracetam \| Otilonium bromide \| Ethyl cinnamate \| Lanthanum(III) chloride heptahydrate \| Diltiazem hydrochloride \| L-Ascorbic acid \| Nimodipine \| 1,2,4-Trihydroxybenzene

關(guān)鍵字： SB262470|||SB 262470A|||NPS 2143|||2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羥基丙氧基]苯腈|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域科學家的研究提供專業(yè)的產(chǎn)品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(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、生命科學試劑盒等，此外，我們還建設有CADD（計算機輔助藥物設計）研究中心、藥理實驗室、藥化合成平臺三大技術(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、快速高效的全球供應鏈和專業(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）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年營業(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,分子砌塊,生物技術(shù)服務	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務

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公司成立：12年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責任公司(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
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