| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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Tecalcet (KRN-568; NPS-R-568; R-568) is a novel, potent, orally bioactive calcimimetic compound/calcium channel agonist that can be potentially used for the treatment of hyperparathyroidism, postmenopausal symptom. It stimulates the calcium-sensing receptor (CaSR) allosterically and favorably. In rats with severe secondary hyperparathyroidism, NPS R-568 prevents parathyroid hyperplasia. In rats suffering from mild to severe secondary hyperparathyroidism due to diet or renal disease, NPS R-568 reduces plasma PTH. In uremic rats, osteitis fibrosa is stopped or reversed by NPS R-568.
| 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].
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| 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].
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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 |
| References |
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| Molecular Formula |
C18H23CL2NO
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|---|---|
| Molecular Weight |
340.287323236465
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| Exact Mass |
339.12
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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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| Appearance |
Solid powder
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| SMILES |
C[C@H](C1=CC(=CC=C1)OC)NCCCC2=CC=CC=C2Cl.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 |
| 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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