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Submit ReviewNPS 2143 hydrochloride
说明： Selective calcium-sensing receptor (CaSR) antagonist; orally active calcilytic agent
化学名： 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino-2-hydroxypropoxy]benzonitrile hydrochloride
纯度： ≥99% (HPLC)
生物活性 for NPS 2143 hydrochloride
NPS 2143 hydrochloride is a selective Ca2+-sensing receptor antagonist. Blocks increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells (IC50 = 43 nM). Also stimulates parathyroid hormone secretion from bovine parathyroid cells (EC50 = 41 nM). Orally active calcilytic compound.
化合物库 for NPS 2143 hydrochloride
NPS 2143 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for NPS 2143 hydrochloride
| 分子量 | 445.38 |
| 公式 | C24H25ClN2O2.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 324523-20-8 |
| PubChem ID | 9868131 |
| InChI Key | ZEBNDUQLNGYBNL-VEIFNGETSA-N |
| Smiles | CC(NC[C@@H](O)COC3=C(C#N)C(Cl)=CC=C3)(C)CC2=CC1=CC=CC=C1C=C2.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for NPS 2143 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.54 | 100 | |
| ethanol | 4.45 | 10 |
制备储备液 for NPS 2143 hydrochloride
以下数据基于产品分子量 445.38。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.25 mL | 11.23 mL | 22.45 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.49 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.25 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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产品说明书 for NPS 2143 hydrochloride
参考文献 for NPS 2143 hydrochloride
参考文献是支持产品生物活性的出版物。
Nemeth et al (2001) Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J.Pharmacol.Exp.Ther. 299 323 PMID: 11561095
Nemeth (2002) The search for calcium receptor antagonists (calcilytics). J.Mol.Endocrinol. 29 15 PMID: 12200226
Huang and Breitwieser (2007) Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J.Biol.Chem. 282 9517 PMID: 17284438
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关键词: NPS 2143 hydrochloride, NPS 2143 hydrochloride supplier, calcium, Ca2+, sensing, receptors, CaSR, antagonists, orally, active, calcilytics, NPS2143, Calcium-Sensing, Receptor, 3626, Tocris Bioscience
13 篇 NPS 2143 hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 NPS 2143 hydrochloride 的部分引用包括：
Kim et al (2014) Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection. Ann Clin Transl Neurol 1 851 PMID: 25540800
Donald T et al (2021) Study of the Expression and Function of Calcium-Sensing Receptor in Human Skeletal Muscle. Int J Mol Sci 22 PMID: 34298895
Catherine A et al (2022) Calcium-sensing receptor and CPAP-induced neonatal airway hyperreactivity in mice. Pediatr Res 91 1391-1398 PMID: 33958714
Silvia F et al (2022) Regulation of Stanniocalcin Secretion by Calcium and PTHrP in Gilthead Seabream (Sparus aurata). Biology (Basel) 11 PMID: 35741384
Yamamura et al (2015) Inhibition of Excessive Cell Proliferation by Calcilytics in Idiopathic Pulmonary Arterial Hypertension. Sci Transl Med 10 e0138384 PMID: 26375676
Yarova et al (2015) Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. Diabetologia 7 284ra60 PMID: 25904744
Yamamura et al (2012) Enhanced Ca(2+)-sensing receptor function in idiopathic pulmonary arterial hypertension. Circ Res 111 469 PMID: 22730443
Bidhan C et al (2020) l-ornithine activates Ca2+ signaling to exert its protective function on human proximal tubular cells. Cell Signal 67 109484 PMID: 31770578
Diakogiannaki et al (2013) Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor. Front Mol Neurosci 56 2688 PMID: 24045836
Ian P et al (2023) Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation. Cell Signal 107 110676 PMID: 37028778
Dai et al (2014) Calcium deficiency-induced and TRP channel-regulated IGF1R-PI3K-Akt signaling regulates abnormal epithelial cell proliferation. Cell Death Differ 21 568 PMID: 24336047
Zhang et al (2019) Mechanisms of Pancreatic Injury Induced by Basic Amino Acids Differ Between L-Arginine, L-Ornithine, and L-Histidine. Front Physiol 9 1922 PMID: 30697165
Jouret et al (2013) Activation of the Ca2+-sensing receptor induces deposition of tight junction components to the epithelial cell plasma membrane. J Cell Sci 126 5132 PMID: 24013548
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