CAS NO: | 729610-18-8 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 336.9 |
Cas No. | 729610-18-8 |
Formula | C21H20N2·HCl |
Solubility | ≤15mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide |
Chemical Name | N-[(1R)-1-(1-naphthalenyl)ethyl]-1H-indole-2-methanamine, monohydrochloride |
Canonical SMILES | C[C@H](C1=C(C=CC=C2)C2=CC=C1)NCC3=CC4=CC=CC=C4N3.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Calindol is an activator of the calcium-sensing receptor (CaSR).
The extracellular calciumsensing receptor (CaSR), a G protein-coupled receptor (GPCR), senses extracellular calcium[Ca2+]e and regulates calciumion homeostasis. The CaSR has a long amino terminal tail typical of family 3 of GPCRs including the metabotropic glutamate receptors, the c-aminobutyric acid B receptor and certain pheromone and taste receptors. CaSR cDNA has been cloned fromsuch tissues as the parathyroid, thyroid, kidney as well as brain. The CaSR at the surface can detect and respond to small changes of circulating [Ca2+]e in the particular case of the parathyroid cell.
In vitro: Previous study found that calindol could display improved calcimimetic activity compared to its N2-(2-chloro-(or 4-fluoro-)benzyl)-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamine analogs as well as stereoselectivity. In the presence of 2 mM Ca(2+), calindol was able to stimulate [(3)H]inositol phosphates accumulation with an EC(50) of 1.0+/-0.1 or 0.31+/-0.05 μM in cells expressing the rat or the human CaSR, respectively. Therefore, such calcimimetic activities of this novel compound were shown to be because of a specific interaction with the CaSR [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Kessler, A. ,Faure, H.,Petrel, C., et al. N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: Development of calindol as a new calcimimetic acting at the calcium sensing receptor. Bioorganic & Medicinal Chemistry Letters 14(12), 3345-3349 (2004).