Cinacalcet (AMG-073) HCl - 10mM in DMSO , Calcium sensing receptor positive allosteric modulator, CAS No.364782-34-3, Calcium sensing receptor positive allosteric modulator

CAS: 364782-34-3 Cat. No.: C409164 Peso molecular: 393.87 Número EC: 620-490-5 PubChem CID: 156418

GRADE & PURITY 10mM in DMSO

Synonyms

(R)-N-(1-(naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Cinacalcet (AMG-073) HCl Cinacalcet (AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism.
In vitro

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

(R)-N-(1-(naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Cinacalcet (AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

POSITIVE ALLOSTERIC MODULATOR

Mecanismo de acción

Calcium sensing receptor positive allosteric modulator

Nombres e identificadores

• Isómeros SMILES: C[C@H](C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl
• PubChem CID: 156418
• Peso molecular: 393.87

Objetivos asociados (humanos)

CASR Tclin Extracellular calcium-sensing receptor (1 Activities)

Discover Target: CASR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)