| CAS NO: | 364782-34-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 393.87 |
|---|---|
| Formula | C22H22F3N.HCl |
| CAS No. | 364782-34-3 (HCl salt) |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 79 mg/mL (200.6 mM) |
| Water: <1 mg/mL | |
| Ethanol: 33 mg/mL (83.8 mM) | |
| Solubility (In vivo) | 30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL |
| Synonyms | AMG073 HCl; Cinacalcet Hydrochloride; Sensipar; AMG-073 HCl; AMG 073 HCl; KRN1493; KRN-1493; Cinacalcet HCl; Mimpara; Regpara; cinacalcet; cinacalcet hydrochloride; Hydrochloride, Cinacalcet; KRN 1493; Chemical Name: N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine;hydrochloride SMILES Code: C[C@H](C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl |
| In Vitro | In vitro activity: AMG-073 represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium. AMG-073 has potential advantages as a therapy for secondary hyperparathyroidism because it mimics the effects of extracellular calcium to suppress PTH secretion, even in the presence of hyperphosphatemia, without the risk of causing hypercalcemia and/or hyperphosphatemia. AMG-073 produces a concentration-dependent increase in cytoplasmic calcium in human embryonic kidney cells expressing the CaSR. In bovine parathyroid cells and a buffer containing calcium 0.5 mM, AMG 073 (3 nM – 1 μM) produces a concentration-dependent decrease in PTH levels with IC50 of 27 nM. |
|---|---|
| In Vivo | AMG-073 orally administrated to normal rats at dose of 1, 3, 10, and 30 mg/kg in 20% sulfobutyl ether β-cyclodextrin sodium produces a significant dose-dependent reduction in PTH levels for 1 to 4 hours after administration. At 8 hours, the 10- and 30-mg/kg doses of AMG-073 produces significant reductions in PTH levels compared with controls that disappears by 24 hours. Significant dose-dependent reduction in serum calcium levels are observed at 4, 8, and 24 hours after oral administration of AMG-073 3, 10, and 30 mg/kg, respectively. A transient reduction in serum phosphorus levels is observed only with the highest dose of AMG-073. In addition, increased calcitonin levels that paralleled PTH suppression are observed with AMG-073 40 mg/kg in rats. As in normal rats, a rapid dose-dependent reduction in PTH and calcium levels is observed in 5 of 6 nephrectomized rats after oral administration of AMG-073. In addition, oral AMG-073 at 5 and 10 mg/kg for 4 weeks significantly reduces parathyroid weight compared with controls. |
| Animal model | Rats |
| Formulation & Dosage | Dissolved in 20% sulfobutyl ether β-cyclodextrin sodium; 1, 3, 10, and 30 mg/kg; oral |
| References | Kidney Int Suppl. 2003 Jun;(85):S91-6; Clin Ther. 2005 Nov;27(11):1725-51. |
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