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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
NPS-2143 Hydrochloride
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
324523-20-8
- 规格：
1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ¥386.00 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ¥800.00 |
| 规格： | 10mg | 产品价格： | ¥1222.00 |
| 规格： | 25mg | 产品价格： | ¥2078.00 |
| 规格： | 50mg | 产品价格： | ¥3330.00 |
| 规格： | 100mg | 产品价格： | ¥4666.00 |
| CAS | 324523-20-8 |
| 英文名称 | NPS-2143 Hydrochloride |
| 别名 | SB-262470A hydrochloride |
| 分子式 | C24H25ClN2O2·HCl |
| 分子量 | 445.38 |
| 规格 | 1mg ; 5mg ; 10mg ; 25mg ; 50mg ; 100mg |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| EC | 803-657-9 |
| SMILES | N#CC1=C(OC[C@@H](CNC(C)(C)CC2=CC=C3C=CC=CC3=C2)O)C=CC=C1Cl.[H]Cl |
| InChIKey | ZEBNDUQLNGYBNL-VEIFNGETSA-N |
| InChI | InChI=1S/C24H25ClN2O2.ClH/c1-24(2，13-17-10-11-18-6-3-4-7-19(18)12-17)27-15-20(28)16-29-23-9-5-8-22(25)21(23)14-26;/h3-12，20，27-28H，13，15-16H2，1-2H3;1H/t20-;/m1./s1 |
| PubChem CID | 9868131 |
| 靶点 | CaSR |
| 通路 | GPCR & G Protein |
| 背景说明 | 是选择性的Ca(2+)受体拮抗剂。 |
| 生物活性 | NPS-2143 hydrochloride (SB-262470A hydrochloride)， an orally active calcilytic agent， is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor[1][2]. |
| In Vitro | First we characterized the sensitivity of loss - or gain - of - function CaR mutants to proteasome inhibition by MG132. The stabilization of loss - of - function mutants and insensitivity of gain - of - function mutants to MG132 suggests that receptor sensitivity to calcium influences susceptibility to proteasomal degradation.Second， we used the allosteric activator NPS R - 568 and antagonist NPS 2143 to promote the active and inactive conformations of wild type CaR， respectively. Overnight culture in NPS R - 568 increased expression of CaR， whereas NPS 2143 had the opposite effect. NPS R - 568 and NPS 2143 differentially regulated maturation and cell surface expression of wild type CaR， directly affecting maximal signaling responses. NPS R - 568 rescued expression of loss - of - function CaR mutants， increasing plasma membrane expression and ERK1/2 phosphorylation in response to 5 mM Ca(2+).[1]。 |
| In Vivo | When administered as a single agent to rats， the previously reported calcium receptor antagonist 3 elicited a sustained elevation of plasma PTH resulting in no increase in overall bone mineral density. The lack of a bone building effect for analogue 3 was attributed to the large volume of distribution (V(dss)(rat) = 11 L/kg)， producing a protracted plasma PTH profile.Antagonist 12 elicited a rapid and transient increase in circulating levels of PTH following oral dosing of the ester prodrug 11 in the dog. The magnitude and duration of the increases in plasma levels of PTH would be expected to stimulate new bone formation.[2]。 |
| 数据来源文献 | [1]. Huang Y， Breitwieser GE. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J Biol Chem. 2007 Mar 30;282(13):9517-25 [2]. Marquis， Robert W.; Lago， Amparo M.; Callahan， James F.;Antagonists of the Calcium Receptor. 2. Amino Alcohol-Based Parathyroid Hormone Secretagogues. Journal of Medicinal Chemistry (2009)， 52(21)， 6599-6605. [3]. Yamamura A， Guo Q， Yamamura H， Zimnicka AM， Pohl NM， Smith KA， Fernandez RA， Zeifman A， Makino A， Dong H， Yuan JX.Enhanced Ca2+-sensing receptor function in idiopathic pulmonary arterial hypertension.Circ Res. 2012 Aug 3;111(4):469-81. Epub 2012 Jun 22. [4]. Nakajima S， Hira T， Hara H.Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells.Mol Nutr Food Res. 2012 May;56(5):753-60. [5]. Davey AE， Leach K， Valant C， Conigrave AD， Sexton PM， Christopoulos A.Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.Endocrinology. 2012 Mar;153(3):1232-41. Epub 2011 Dec 30. [6]. Nemeth EF， et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|2.2453mL|11.2264mL|22.4527mL|$$|5mM|0.4491mL|2.2453mL|4.4905mL|$$|10mM|0.2245mL|1.1226mL|2.2453mL| |
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