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网站主页 化工产品目录 生物化工 抑制剂 G蛋白偶联受体(GPCR & G Protein) CaSR 拮抗剂 2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈 化合物 NPS 2143
  • 化合物 NPS 2143|T1730|TargetMol

化合物 NPS 2143|T1730|TargetMol

NPS-2143
284035-33-2
￥228 1mg 起订
￥497 5mg 起订
￥729 10mg 起订
上海 更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 NPS 2143
英文名称：
NPS-2143
CAS号：
284035-33-2
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
98.24%
产品类别：
抑制剂
货号：
T1730

Product Introduction

Bioactivity

NameNPS-2143
DescriptionNPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.
Kinase AssayThis 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 vitroNPS 2143刺激牛甲状旁腺细胞分泌甲状旁腺激素（PTH）,EC50 为41 nM。此外,NPS 2143会阻断拟钙剂NPS R-467对PTH从牛甲状旁腺细胞分泌的抑制作用以及细胞外Ca2+对异丙肾上腺素刺激的环AMP形成增加的抑制作用。表达人Ca2+受体的HEK 293细胞中,NPS 2143阻断Ca2+受体激活诱发的细胞质Ca2+浓度增加,IC50为43 nM。 在短暂表达hCaSRs的HEK-293细胞中,NPS 2143通过有效抑制GSH (数据未显示)和γ-Glu-Val-Gly活性,明显抑制厚味味觉。
In vivo在血压正常的大鼠体内,静脉注射NPS 2143（1 mg/kg） 在甲状旁腺存在的情况下显著增加平均动脉血压（MAP）.在大鼠体内,NPS 2143导致血浆PTH水平迅速增加4-5倍,并且血浆Ca 2+水平也瞬时升高.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 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.
KeywordsSB-262470A | Inhibitor | inhibit | Calcium-sensing receptor | SB 262470 | CaSR | NPS-2143 | NPS2143 | SB-262470
Inhibitors RelatedNisoldipine | 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
SB262470|||SB 262470A|||NPS 2143|||2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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