化合物 NPS 2143|T1730|TargetMol

價(jià)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	2024-09-29

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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(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: 98.24%	產(chǎn)品類別: 抑制劑
貨號(hào): T1730

Product Introduction

Bioactivity

名稱	NPS-2143
描述	NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.
激酶實(shí)驗(yàn)	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.
體外活性	NPS 2143刺激牛甲狀旁腺細(xì)胞分泌甲狀旁腺激素（PTH）,EC50 為41 nM。此外,NPS 2143會(huì)阻斷擬鈣劑NPS R-467對(duì)PTH從牛甲狀旁腺細(xì)胞分泌的抑制作用以及細(xì)胞外Ca2+對(duì)異丙腎上腺素刺激的環(huán)AMP形成增加的抑制作用。表達(dá)人Ca2+受體的HEK 293細(xì)胞中,NPS 2143阻斷Ca2+受體激活誘發(fā)的細(xì)胞質(zhì)Ca2+濃度增加,IC50為43 nM。在短暫表達(dá)hCaSRs的HEK-293細(xì)胞中,NPS 2143通過(guò)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。
體內(nèi)活性	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(dòng)脈血壓（MAP）.在大鼠體內(nèi),NPS 2143導(dǎo)致血漿PTH水平迅速增加4-5倍,并且血漿Ca 2+水平也瞬時(shí)升高.
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 : < 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.
關(guān)鍵字	SB-262470A \| Inhibitor \| inhibit \| Calcium-sensing receptor \| SB 262470 \| CaSR \| NPS-2143 \| NPS2143 \| SB-262470
相關(guān)產(chǎn)品	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|||NPS 2143|||SB 262470A|||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

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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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