Calindol (hydrochloride) |
Katalog-Nr.GC12620 |
activator of the calcium-sensing receptor (CaSR)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 729610-18-8
Sample solution is provided at 25 µL, 10mM.
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).
Cas No. | 729610-18-8 | SDF | |
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 | ||
Formula | C21H20N2 • HCl | M.Wt | 336.9 |
Löslichkeit | ≤15mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.9682 mL | 14.8412 mL | 29.6824 mL |
5 mM | 0.5936 mL | 2.9682 mL | 5.9365 mL |
10 mM | 0.2968 mL | 1.4841 mL | 2.9682 mL |
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Calculation results:
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5
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