Cinacalcet HCl
Cinacalcet hydrochloride
CAS: 364782-34-3
Molecular Formula: C22H23ClF3N
Cinacalcet HCl - Names and Identifiers
| Name | Cinacalcet hydrochloride |
| Synonyms | calcimimetics Cinacalcet HCl Cinacalcet Hydrochloride Cinacalcet hydrochloride (R)-Cinacalcet Hydrochloride (R)-N-(3-(3-(trifluoromethyl)phenyl)propyl)-1--(1-napthyl)ethylamine Hydrochloride N-((1R)-1-(1-Naphthyl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine hydrochloride (aR)-a-Methyl-N-[3-[3-(trifluoromethyl)phenyl)propyl]-1-napthalenemethanamine Hydrochloride |
| CAS | 364782-34-3 |
| EINECS | 620-490-5 |
| InChI | InChI=1/C22H22F3N.ClH/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25;/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3;1H/t16-;/m1./s1 |
Cinacalcet HCl - Physico-chemical Properties
| Molecular Formula | C22H23ClF3N |
| Molar Mass | 393.88 |
| Melting Point | 175-177°C |
| Solubility | Soluble in water (1 mg/ml at 25 °C), DMSO (79 mg/ml at 25 °C), ethanol (33 mg/ml |
| Storage Condition | Inert atmosphere,2-8°C |
| Use | An allosteric activator of CaSR |
| In vitro study | Cinacalcet HCl represents a new class of compounds used to treat hyperthyroidism, is a calcimimetic, by increasing the parathyroid calcium-sensing receptor (CaR) it is sensitive to extracellular calcium ions and reduces the synthesis and secretion of parathyroid hormone (PTH). Cinacalcet HCl has a potential advantage as a therapeutic agent for secondary hyperparathyroidism because it mimics the action of extracellular calcium ions to inhibit PTH secretion, even in the presence of hyperphosphatemia, there is also no risk of causing hypercalcemia and/or hyperphosphatemia. Cinacalcet HCl produces a concentration-dependent increase in cytoplasmic calcium in CaSR-expressing human embryonic kidney cells. In bovine parathyroid cells and a buffer containing calcium 0.5 mM,AMG 073 (3 nM - 1 μm) produced a concentration-dependent decrease in PTH levels with an IC50 of 27 nM. |
| In vivo study | Cinacalcet HCl was administered orally to normal rats at doses of 1, 3, 10, and 30 mg/kg in 20% sodium sulfobutyl ether β-cyclodextrin, after 1 to 4 hours of administration, there was a significant dose-dependent reduction in PTH levels. At 8 hours, compared with the control group, cinacalcet HCl at doses of 10 and 30 mg/kg produced a significant reduction in PTH levels, which disappeared at 24 h. After oral administration of Cinacalcet HCl at doses of 3, 10, and 30 mg/kg, significant reductions in serum calcium levels were observed after 4, 8, and 24 hours, respectively. A transient decrease in serum phosphorus levels was observed only at high doses of Cinacalcet HCl. In addition, in rats, at 40 mg/kg Cinacalcet HCl, with the inhibition of PTH, an increase in the level of calcitonin can be observed. In normal rats, a rapid dose-dependent decrease in PTH and calcium levels was able to be observed in 5 of 6 nephrectomized rats after oral administration of Cinacalcet HCl. In addition, oral administration of 5 and 10 mg/kg Cinacalcet HCl for 4 weeks significantly reduced the weight of parathyroid glands compared with the control group. |
Cinacalcet HCl - Risk and Safety
| Safety Description | 24/25 - Avoid contact with skin and eyes. |
| HS Code | 29214990 |
Cinacalcet HCl - Reference Information
| introduction | sinacase hydrochloride is a specific drug to control hyperparathyroidism and inhibit parathyroid hormone PTH, and has now become a first-line drug in most parts of the country. However, because it is a new drug, doctors in many places do not have much experience in medication, and because many patients have been taking Indian generic drugs, the instructions have not been seen, resulting in blind medication and the effect of medication is not very good. |
| effect | cinacalcet is a calcium-like agent, which can improve the disorder of bone metabolism in uremia and delay the progression of vascular and valve calcification in dialysis patients. However, long-term use of cinacalcet can also cause side effects such as nausea and vomiting, hypocalcemia, and excessive suppression of parathyroid hormone (PTH). The characteristic of Sinacase is not only to reduce the serum PTH level, but also to reduce the serum calcium, serum phosphorus and serum calcium and phosphorus product levels. It can inhibit the occurrence and progression of cardiovascular diseases caused by ectopic calcification. |
| adverse reactions | adverse reactions of parathyroid hormone hydrochloride, mainly: nausea and vomiting (21.6%,124/573 cases), stomach discomfort (18.7%,107/573 cases) and other digestive system symptoms. |
| Biological activity | Cinacalcet (AMG-073) HCl is a new compound used to treat hyperparathyroidism. |
| Target | Value |
| CaSR () | 2.8 μM(EC50) |
| use | new compound has definite curative effect on patients with secondary hyperparathyroidism undergoing dialysis due to chronic kidney disease, and has good safety, tolerance and convenient administration. it has been widely used in clinic. |
Last Update：2024-04-09 15:16:50
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