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NPS-2143  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥100 mg/mL）
产品描述：基本信息 产品编号： N10512  产品名称： NPS-2143 CAS: 284035-33-2   储存条件 粉末 -20℃ 四年     分子式： C24H25ClN2O2 溶于液体 -80℃ 6个月 分子量： 408.92 -20℃ 1个月 化学名：  2-CHLORO-6-[(2R)-3-[[1,1-DIMETHYL-2-(2-NAPHTHALENYL)ETHYL]AMINO]-2-HYDROXYPROPOXY]BENZONITRILE Solubility (25°C)：   体外:   DMSO 82mg/mL (200.52mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 2% DMSO+corn oil 10mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.4455mL 12.2273mL 24.4547mL 5mM 0.4891mL 2.4455mL 4.8909mL 10mM 0.2445mL 1.2227mL 2.4455mL 50mM 0.0489mL 0.2445mL 0.4891mL 生物活性 产品描述 一种口服活性溶钙剂， 选择性的钙敏感受体 (CaSR) 拮抗剂。NPS-2143 (SB-262470A) 通过激活表达人 Ca2+ 受体的 HEK 293 细胞中的 Ca2+ 受体而引起的胞浆 Ca2+ 浓度增加 (IC50=43nM)。 靶点 43nM (Ca2+receptor)   体外研究 NPS-2143 (SB-262470A) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41nM.Moreover,NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+on isoproterenol-stimulated increases in cyclic AMP formation.In HEK 293 cells transiently expressing hCaSRs,NPS-2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH and γ-Glu-Val-Gly.A recent study shows that NPS-2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells. 体内研究 NPS-2143 (SB-262470A) results in a rapid 4-to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+levels in rats.In normotensive rats,NPS-2143 administration (1mg/kg,i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands. 推荐实验方法(仅供参考) 激酶实验： 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 1.0mM to 1.75mM.NPS-2143 is tested individually at a concentration of 100μg/mL (20μM-80μM) 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.   动物实验:   Rats:On the day of study,the rats are infused intravenously (0.1mL/kg·min) for 120 min with NPS-2143 (0.1μmol/kg·min) or vehicle,a 20% aqueous solution of 2-hydroxypropyl-β-cyclodextrin.Blood samples (0.5mL) are collected before and at various times after the start of the infusion for measurements of plasma levels of PTH and Ca2+.To prevent excessive blood volume loss during the course of the experiment,for each blood sample the erythrocyte pellet is resuspended in an equal volume of normal rat plasma and reinjected.Plasma levels of Ca2+are measured immediately after collection using a model 634 ionized calcium analyzer.PTH levels are measured using the Immutopics rat PTH(1-34) immunoradiometric assay kit.
保存条件：-20℃

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