Description
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 . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 729610-18-8
Molecular Weight: 336.86
Formula: C21H21ClN2
Chemical Name: [(1H-indol-2-yl)methyl][(1R)-1-(naphthalen-1-yl)ethyl]amine hydrochloride
Smiles: Cl.C[C@@H](NCC1=CC2=CC=CC=C2N1)C1C=CC=C2C=CC=CC2=1
InChiKey: KFILKQPBQZIRST-XFULWGLBSA-N
InChi: InChI=1S/C21H20N2.ClH/c1-15(19-11-6-9-16-7-2-4-10-20(16)19)22-14-18-13-17-8-3-5-12-21(17)23-18;/h2-13,15,22-23H,14H2,1H3;1H/t15-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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