Cinacalcet hydrochloride

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Description: Allosteric Calcium-sensing receptor (CaSR) agonist; also CYP2D2 inhibitor and Ca2+ channel blocker; orally bioavailable
Alternative Names: AMG 073
Chemical Name: N-[(1R)-1-(1-Naphthyl)ethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews

Biological Activity for Cinacalcet hydrochloride

Cinacalcet hydrochloride is a calcium-sensing receptor (CaSR) allosteric agonist. Activates CaSR signaling in cellular proliferation and phosphatidylinositol (PI) hydrolysis assays. Reduces serum parathyroid hormone levels in rats. Also potent CYP2D2 inhibitor (IC50 = 87 nM) and L-type calcium channel blocker. Orally bioavailable.

Compound Libraries for Cinacalcet hydrochloride

Cinacalcet hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Cinacalcet hydrochloride

M. Wt 393.87
Formula C22H22F3N.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 364782-34-3
PubChem ID 156418
InChI Key QANQWUQOEJZMLL-PKLMIRHRSA-N
Smiles C[C@H](C1=CC=CC2=C1C=CC=C2)NCCCC3=CC(C(F)(F)F)=CC=C3.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Cinacalcet hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.39 100

Preparing Stock Solutions for Cinacalcet hydrochloride

The following data is based on the product molecular weight 393.87. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.54 mL 12.69 mL 25.39 mL
5 mM 0.51 mL 2.54 mL 5.08 mL
10 mM 0.25 mL 1.27 mL 2.54 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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Product Datasheets for Cinacalcet hydrochloride

References for Cinacalcet hydrochloride

References are publications that support the biological activity of the product.

Goodman et al (2002) The calcimimetic agent AMG 073 lowers plasma parathyroid hormone levels in hemodialysis patients with secondary hyperparathyroidism. J.Am.Soc.Nephrol. 13 1017 PMID: 11912261

Ma et al (2011) Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J.Pharmacol.Exp.Ther. 337 275 PMID: 21239511


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Keywords: Cinacalcet hydrochloride, Cinacalcet hydrochloride supplier, AMG073, calcium-sensing, receptor, CaSR, allosteric, agonists, agonism, calcimimetic, CYP2D2, inhibitors, inhibits, L-type, calcium, channel, blockers, Sensipar, AMG, 073, Calcium-Sensing, Receptor, Cytochrome, P450, Cav1.x, Channels, 6170, Tocris Bioscience

2 Citations for Cinacalcet hydrochloride

Citations are publications that use Tocris products. Selected citations for Cinacalcet hydrochloride include:

Ian P et al (2023) Asymmetric dimethylarginine positively modulates calcium-sensing receptor signalling to promote lipid accumulation. Cell Signal 107 110676 PMID: 37028778

Stephen D et al (2021) Area Postrema Cell Types that Mediate Nausea-Associated Behaviors. Neuron 109 461-472.e5 PMID: 33278342


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