Cinacalcet HCl

SKU: orb1305532

Description

Cinacalcet hydrochloride is a calcimimetic agent that sensitizes the parathyroid calcium-sensing receptor, thereby lowering parathyroid hormone and serum calcium levels. It is widely used in research on secondary hyperparathyroidism, enabling both in vitro receptor studies and in vivo animal models of mineral metabolism disorders.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 364782-34-3
• MW: 393.9
• Purity: >98%
• Formula: C₂₂H₂₂F₃N • HCl
• SMILES: C[C@H](c1cccc2ccccc12)NCCCc1cc(ccc1)C(F)(F)F.Cl
• Target: GPCR
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Water (up to 5 mg/ml with warming)

Bioactivity

• Target IC50:
  CaSR:2.8 μM(EC50)
• In Vivo:
  Cinacalcet HCl induces a concentration-dependent increase in cytoplasmic calcium levels in human embryonic kidney cells expressing the CaSR (Calcium-Sensing Receptor). Furthermore, in bovine parathyroid cells and a buffer containing 0.5 mM calcium, a concentration-dependent decrease in PTH (Parathyroid Hormone) levels was observed when treated with AMG 073 (Cinacalcet) concentrations ranging from 3 nM to 1 μM, achieving an IC50 of 27 nM.
• In Vitro:
  Significant dose-dependent reductions in serum calcium levels were observed at 4, 8, and 24 hours post-oral administration of AMG-073 at dosages of 3, 10, and 30 mg/kg. A transient decrease in serum phosphorus levels was noted only with the highest dosage of AMG-073. Oral administration of Cinacalcet HCl at 1, 3, 10, and 30 mg/kg in 20% sulfobutylether-β-cyclodextrin sodium to normal rats induced a significant dose-dependent reduction in PTH levels within 1 to 4 hours. By 8 hours post-dosing, a significant reduction in PTH levels was observed with 10 and 30 mg/kg doses compared to the control group, with this effect dissipating after 24 hours. Additionally, an increase in calcitonin levels accompanying PTH suppression was observed with 40 mg/kg AMG-073 in rats. Similar to normal rats, a rapid dose-dependent reduction in PTH and calcium levels was noted in five out of six nephrectomized rats following oral AMG-073 administration. Furthermore, oral administration of 5 and 10 mg/kg Cinacalcet HCl for 4 weeks significantly reduced the weight of the parathyroid gland compared to the control group.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG 073; KRN 1493; Mimpara; Sensipar

Compound Identifiers

PubChem CID

156418