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Cinacalcet hydrochloride

Catalog No. T2406   CAS 364782-34-3
Synonyms: AMG-073 HCl, Cinacalcet HCl, AMG-073 hydrochloride, Cinacalcet

Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and CALCIMIMETIC AGENT that increases the sensitivity of PARATHYROID GLAND calcium-sensing receptors to serum calcium. This action reduces parathyroid hormone secretion and decreases serum calcium in the treatment of PARATHYROID DISEASES.

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Cinacalcet hydrochloride Chemical Structure
Cinacalcet hydrochloride, CAS 364782-34-3
Pack Size Availability Price/USD Quantity
10 mg In stock $ 43.00
25 mg In stock $ 64.00
50 mg In stock $ 80.00
100 mg In stock $ 147.00
200 mg In stock $ 195.00
500 mg In stock $ 326.00
1 mL * 10 mM (in DMSO) In stock $ 48.00
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Purity: 99.94%
Purity: 99.9%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and CALCIMIMETIC AGENT that increases the sensitivity of PARATHYROID GLAND calcium-sensing receptors to serum calcium. This action reduces parathyroid hormone secretion and decreases serum calcium in the treatment of PARATHYROID DISEASES.
Targets&IC50 CaSR:2.8 μM(EC50)
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.
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.
Synonyms AMG-073 HCl, Cinacalcet HCl, AMG-073 hydrochloride, Cinacalcet
Molecular Weight 393.87
Formula C22H23ClF3N
CAS No. 364782-34-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39.4 mg/mL (100 mM)

TargetMolReferences and Literature

1. Ureña P, et al. Kidney Int Suppl, 2003, (85), S91-96. 2. Dong BJ. Clin Ther, 2005, 27(11), 1725-1751.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library GPCR Compound Library EMA Approved Drug Library FDA-Approved Drug Library Endocrinology-Hormone Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library

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NPS-2143 hydrochloride Ronacaleret HCl SB-423562 Calhex 231 hydrochloride Upacicalcet HCl CaSR antagonist-1 NPS-2143 Poly-D-lysine hydrobromide (MW 30000-70000)

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Keywords

Cinacalcet hydrochloride 364782-34-3 GPCR/G Protein CaSR AMG-073 AMG-073 HCl Endogenous Metabolite Cinacalcet HCl Cinacalcet Hydrochloride Calcium-sensing receptor Inhibitor AMG 073 AMG-073 hydrochloride AMG 073 Hydrochloride AMG073 Hydrochloride AMG-073 Hydrochloride Cinacalcet inhibit AMG073 inhibitor

 

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