| Name | Cinacalcet hydrochloride |
| Description | Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and calcimimetic agent that enhances the sensitivity of parathyroid gland calcium-sensing receptors to serum calcium, thereby reducing parathyroid hormone secretion and decreasing serum calcium in the treatment of parathyroid diseases. |
| In vitro | Significant dose-dependent reductions in serum calcium levels were observed at 4, 8, and 24 hours post-oral administration of AMG-073 at dosages of 3, 10, and 30 mg/kg. A transient decrease in serum phosphorus levels was noted only with the highest dosage of AMG-073. Oral administration of Cinacalcet HCl at 1, 3, 10, and 30 mg/kg in 20% sulfobutylether-β-cyclodextrin sodium to normal rats induced a significant dose-dependent reduction in PTH levels within 1 to 4 hours. By 8 hours post-dosing, a significant reduction in PTH levels was observed with 10 and 30 mg/kg doses compared to the control group, with this effect dissipating after 24 hours. Additionally, an increase in calcitonin levels accompanying PTH suppression was observed with 40 mg/kg AMG-073 in rats. Similar to normal rats, a rapid dose-dependent reduction in PTH and calcium levels was noted in five out of six nephrectomized rats following oral AMG-073 administration. Furthermore, oral administration of 5 and 10 mg/kg Cinacalcet HCl for 4 weeks significantly reduced the weight of the parathyroid gland compared to the control group. |
| In vivo | Cinacalcet HCl induces a concentration-dependent increase in cytoplasmic calcium levels in human embryonic kidney cells expressing the CaSR (Calcium-Sensing Receptor). Furthermore, in bovine parathyroid cells and a buffer containing 0.5 mM calcium, a concentration-dependent decrease in PTH (Parathyroid Hormone) levels was observed when treated with AMG 073 (Cinacalcet) concentrations ranging from 3 nM to 1 μM, achieving an IC50 of 27 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 260 mg/mL (660.12 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.08 mM), Sonication is recommended.
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| Keywords | Cinacalcet | CaSR | Calcium-sensing receptor | AMG073 Hydrochloride | AMG-073 | AMG073 | AMG 073 Hydrochloride | AMG 073 |
| Inhibitors Related | Sucrose | Aceglutamide | Nicotinamide riboside malate | DL-Lysine | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Malic acid | Formamide | Glycerol | Thymidine | Corn starch | Gluconate Calcium |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Orally Active Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
