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Submit ReviewCalhex 231 hydrochloride is a negative allosteric modulator of the calcium sensing receptor (CaSR). Blocks increases in [3H]inositol phosphate levels elicited by wild-type hCasR activation (IC50= 0.39 μM in transiently transfected HEK293 cells).
Calhex 231 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 443.41 |
公式 | C25H27ClN2O.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 2387505-78-2 |
PubChem ID | 11849513 |
InChI Key | KZPHZSFSFANQIS-GRFVZBLOSA-N |
Smiles | O=C(C4=CC=C(Cl)C=C4)N[C@@H](CCCC3)[C@H]3N[C@H](C)C1=C2C(C=CC=C2)=CC=C1.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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 22.17 | 50 |
以下数据基于产品分子量 443.41。 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 |
---|---|---|---|
0.5 mM | 4.51 mL | 22.55 mL | 45.1 mL |
2.5 mM | 0.9 mL | 4.51 mL | 9.02 mL |
5 mM | 0.45 mL | 2.26 mL | 4.51 mL |
25 mM | 0.09 mL | 0.45 mL | 0.9 mL |
参考文献是支持产品生物活性的出版物。
Petrel et al (2003) Modeling and mutagenesis of the binding site of Calhex 231, a novel negative allosteric modulator of the extracellular Ca2+-sensing receptor. J.Biol.Chem. 278 49487 PMID: 14506236
Kessler et al (2006) N1-Benzoyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-chlorophenylcarboxamide (Calhex 231) as a new calcium sensing receptor ligand demonstrating potent calcilytic activity. J.Med.Chem. 49 5119 PMID: 16913701
Weston et al (2008) The expression and function of Ca2+-sensing receptors in rat mesenteric artery; comparative studies using a model of type II diabetes. Br.J.Pharmacol. 154 652 PMID: 18414396
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关键词: Calhex 231 hydrochloride, Calhex 231 hydrochloride supplier, Calhex231, calcilytics, hcasr, calcium-sensing, receptors, negative, allosteric, modulators, nams, Calcium-Sensing, Receptor, 4387, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Calhex 231 hydrochloride 的部分引用包括:
Ulf et al (2022) Macrophages in obesity are characterised by increased IL-1β response to calcium-sensing receptor signals. Int J Obes (Lond) 46 1883-1891 PMID: 35931812
Ian P et al (2023) Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation. Cell Signal 107 110676 PMID: 37028778
Yarova et al (2015) Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. Diabetologia 7 284ra60 PMID: 25904744
Diakogiannaki et al (2013) Oligopeptides stimulate glucagon-like peptide-1 secretion in mice through proton-coupled uptake and the calcium-sensing receptor. Oncotarget 56 2688 PMID: 24045836
Mathias et al (2019) Sensory Axon Growth Requires Spatiotemporal Integration of CaSR and TrkB Signaling. J Neurosci 39 5842-5860 PMID: 31123102
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