Cinacalcet hydrochloride

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Cat.No. 6170 - Cinacalcet hydrochloride | C22H22F3N.HCl | CAS No. 364782-34-3
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
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Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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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References

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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