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Cinacalcet HCl(AMG-073)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cinacalcet HCl(AMG-073)图片
CAS NO:364782-34-3
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)393.87
FormulaC22H22F3N.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

实验参考方法
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 VivoAMG-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 modelRats
Formulation & DosageDissolved 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.