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 Molecular Weight: 393.87 EC Number: 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

Overview

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

Synonyms

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

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

POSITIVE ALLOSTERIC MODULATOR

Mechanism of action

Calcium sensing receptor positive allosteric modulator

Names and Identifiers

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

Associated Targets(Human)

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)