| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Tecalcet HCl's primary target is the calcium-sensing receptor (CaSR). As a calcimimetic, it acts as an agonist of the CaSR, mimicking the effect of extracellular calcium. By activating the CaSR, it inhibits the secretion of parathyroid hormone (PTH), which leads to a reduction in serum calcium levels. This makes it a potential therapeutic agent for hyperparathyroidism.
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| ln Vitro |
Tecalcet (NPS 568, 0.1–100 μM) increases [Ca2+]i in a stereoselective and concentration-dependent way[3].
Tecalcet (NPS 568, 0.1-100 nM) lowers the EC50 value for extracellular Ca21 to 0.61±0.04 mM by moving the concentration-response curve for extracellular Ca2+ to the left without affecting the maximal response[3].
In vitro, Tecalcet HCl acts as a potent agonist of the calcium-sensing receptor. Its activity is assessed in cell-based assays using cells expressing the CaSR. It has been shown to inhibit PTH secretion in parathyroid cells. |
| ln Vivo |
Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits the proliferation of PT cells in rats with renal insufficiency[1].
In vivo, Tecalcet HCl has been studied for its effects on PTH and calcium levels. By activating the CaSR, it reduces PTH secretion, leading to a decrease in serum calcium levels. It has been investigated for the treatment of primary and secondary hyperparathyroidism. |
| Enzyme Assay |
The in vitro activity of Tecalcet HCl is assessed using cell-based assays. Cells expressing the calcium-sensing receptor (e.g., HEK293 cells stably transfected with CaSR) are treated with various concentrations of Tecalcet HCl. The activation of the CaSR is assessed by measuring the increase in intracellular calcium using fluorescent dyes such as Fluo-4 or by measuring the activation of downstream signaling pathways (e.g., MAPK). The inhibition of PTH secretion is assessed in parathyroid cells or in cell lines that secrete PTH.
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| Cell Assay |
For cellular assays, HEK293 cells expressing CaSR or parathyroid cells are cultured in appropriate media. Cells are treated with various concentrations of Tecalcet HCl (typically ranging from 0.1 nM to 10 µM) for different time periods. Intracellular calcium levels are measured using a fluorescence plate reader. PTH secretion is measured by ELISA.
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| Animal Protocol |
10-wk-old Male Sprague-Dawley rats weighing 310-350 g
1.5 and 15 mg/kg Orally twice daily for 4 days In vivo, Tecalcet HCl is typically administered orally to animal models. In studies of hyperparathyroidism, the compound is administered to rats or mice, and blood samples are collected to measure PTH and calcium levels. The efficacy is assessed by the reduction in PTH and serum calcium levels. |
| ADME/Pharmacokinetics |
Tecalcet HCl is orally bioavailable. Its pharmacokinetic profile has been studied in preclinical models. It is expected to be absorbed after oral administration and to have a reasonable half-life. Its metabolism and excretion would require further investigation.
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| Toxicity/Toxicokinetics |
Tecalcet HCl has been studied in clinical trials for the treatment of hyperparathyroidism. As a calcimimetic, it may have side effects related to its mechanism of action, such as hypocalcemia and gastrointestinal effects. Comprehensive toxicological studies are required to establish its full safety profile.
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| References |
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| Additional Infomation |
Tecalcet HCl is a calcimimetic agent that was developed for the treatment of hyperparathyroidism. It is a research compound that has been studied in clinical trials but may not have been approved for marketing. It is a tool for studying the role of the calcium-sensing receptor in calcium homeostasis and for the development of calcimimetic drugs.
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| Molecular Formula |
C18H23CL2NO
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|---|---|
| Molecular Weight |
340.287323236465
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| Exact Mass |
339.116
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| Elemental Analysis |
C, 63.53; H, 6.81; Cl, 20.84; N, 4.12; O, 4.70
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| CAS # |
177172-49-5
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| Related CAS # |
148717-54-8; 177172-49-5 (HCl)
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| PubChem CID |
158796
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| Appearance |
White to off-white solid powder
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| Boiling Point |
416.3ºC at 760 mmHg
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| Flash Point |
205.6ºC
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| Vapour Pressure |
3.86E-07mmHg at 25°C
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| LogP |
5.824
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
286
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@](C1C=C(OC)C=CC=1)(NCCCC1C(Cl)=CC=CC=1)[H].[H]Cl
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| InChi Key |
YJXUXANREVNZLH-PFEQFJNWSA-N
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| InChi Code |
InChI=1S/C18H22ClNO.ClH/c1-14(16-8-5-10-17(13-16)21-2)20-12-6-9-15-7-3-4-11-18(15)19;/h3-5,7-8,10-11,13-14,20H,6,9,12H2,1-2H3;1H/t14-;/m1./s1
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| Chemical Name |
3-(2-chlorophenyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]propan-1-amine;hydrochloride
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| Synonyms |
Tecalcet HCl; KRN-568; NPS-R-568; R-568; KRN568; NPS-R568; R568; Tecalcet hydrochloride; Norcalcin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~146.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (7.35 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9387 mL | 14.6933 mL | 29.3867 mL | |
| 5 mM | 0.5877 mL | 2.9387 mL | 5.8773 mL | |
| 10 mM | 0.2939 mL | 1.4693 mL | 2.9387 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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