Cinacalcet HClCalcium-sensing receptor (CaR) agonist CAS# 364782-34-3 |
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Quality Control & MSDS
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| Cas No. | 364782-34-3 | SDF | Download SDF |
| PubChem ID | 156418 | Appearance | Powder |
| Formula | C22H23ClF3N | M.Wt | 393.87 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | AMG-073 hydrochloride; Cinacalcet | ||
| Solubility | DMSO : ≥ 50 mg/mL (126.95 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine;hydrochloride | ||
| SMILES | [Cl-].C[C@@H](NCCCc1cccc(c1)C(F)(F)F)c2cccc3ccccc23.[H+] | ||
| Standard InChIKey | QANQWUQOEJZMLL-PKLMIRHRSA-N | ||
| Standard InChI | InChI=1S/C22H22F3N.ClH/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25;/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3;1H/t16-;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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. |
Cinacalcet HCl Dilution Calculator
Cinacalcet HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5389 mL | 12.6945 mL | 25.3891 mL | 50.7782 mL | 63.4727 mL |
| 5 mM | 0.5078 mL | 2.5389 mL | 5.0778 mL | 10.1556 mL | 12.6945 mL |
| 10 mM | 0.2539 mL | 1.2695 mL | 2.5389 mL | 5.0778 mL | 6.3473 mL |
| 50 mM | 0.0508 mL | 0.2539 mL | 0.5078 mL | 1.0156 mL | 1.2695 mL |
| 100 mM | 0.0254 mL | 0.1269 mL | 0.2539 mL | 0.5078 mL | 0.6347 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Cinacalcet HCl (AMG 073), the second-generation calcimimetic, is a potent agonist of calcium-sensing receptor (CaR) with an EC50 value of 2.8 μm [1].
Cinacalcet HCl showed to be safe for the secondary hyperparathyroidism treatment. Besides, cinacalcet HCl has been proved to reduce parathyroid hormone (PTH) levels significantly while reducing the calcium x phosphorus product and serum phosphorus levels at the same time [1].
Administered orally with cinacalcet in Rice H-500 tumor bearing mice has shown a significant reduction of blood ionized calcium, serum total calcium concentrations and serum PTHrP levels [2].
References:
[1] Ureña P1, Frazão JM. Calcimimetic agents: review and perspectives. Kidney Int Suppl. 2003 Jun;(85):S91-6.
[2] Colloton M1, Shatzen E, Wiemann B, Starnes C, Scully S, Henley C, Martin D.Cinacalcet attenuates hypercalcemia observed in mice bearing either Rice H-500 Leydig cell or C26-DCT colon tumors. Eur J Pharmacol. 2013 Jul 15;712(1-3):8-15.
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The Effects of Cinacalcet in Older and Younger Patients on Hemodialysis: The Evaluation of Cinacalcet HCl Therapy to Lower Cardiovascular Events (EVOLVE) Trial.[Pubmed:25710802]
Clin J Am Soc Nephrol. 2015 May 7;10(5):791-9.
BACKGROUND AND OBJECTIVES: The calcimimetic cinacalcet reduced the risk of death or cardiovascular (CV) events in older, but not younger, patients with moderate to severe secondary hyperparathyroidism (HPT) who were receiving hemodialysis. To determine whether the lower risk in younger patients might be due to lower baseline CV risk and more frequent use of cointerventions that reduce parathyroid hormone (kidney transplantation, parathyroidectomy, and commercial cinacalcet use), this study examined the effects of cinacalcet in older (>/=65 years, n=1005) and younger (<65 years, n=2878) patients. DESIGN, SETTING, PARTICIPANTS, & MEASUREMENTS: Evaluation of Cinacalcet HCl Therapy to Lower Cardiovascular Events (EVOLVE) was a global, multicenter, randomized placebo-controlled trial in 3883 prevalent patients on hemodialysis, whose outcomes included death, major CV events, and development of severe unremitting HPT. The age subgroup analysis was prespecified. RESULTS: Older patients had higher baseline prevalence of diabetes mellitus and CV comorbidity. Annualized rates of kidney transplantation and parathyroidectomy were >3-fold higher in younger relative to older patients and were more frequent in patients randomized to placebo. In older patients, the adjusted relative hazard (95% confidence interval) for the primary composite (CV) end point (cinacalcet versus placebo) was 0.70 (0.60 to 0.81); in younger patients, the relative hazard was 0.97 (0.86 to 1.09). Corresponding adjusted relative hazards for mortality were 0.68 (0.51 to 0.81) and 0.99 (0.86 to 1.13). Reduction in the risk of severe unremitting HPT was similar in both groups. CONCLUSIONS: In the EVOLVE trial, cinacalcet decreased the risk of death and of major CV events in older, but not younger, patients with moderate to severe HPT who were receiving hemodialysis. Effect modification by age may be partly explained by differences in underlying CV risk and differential application of cointerventions that reduce parathyroid hormone.
Cinacalcet for hemodialyzed patients with or without a high PTH level to control serum calcium and phosphorus: ECO (evaluation of cinacalcet HCl outcome) study.[Pubmed:22790452]
Clin Nephrol. 2012 Aug;78(2):87-92.
BACKGROUND: We investigated the influence of cinacalcet on serum Ca and P in hemodialyzed patients with or without a high PTH level, according to K/DOQI guideline, to control serum Ca and P levels. METHODS: We recruited 130 patients in this prospective cohort study and classified them into Group A (iPTH > 300 pg/ml), Group B (iPTH = 181 - 300 pg/ml), and Group C (iPTH
Cinacalcet, Fibroblast Growth Factor-23, and Cardiovascular Disease in Hemodialysis: The Evaluation of Cinacalcet HCl Therapy to Lower Cardiovascular Events (EVOLVE) Trial.[Pubmed:26059012]
Circulation. 2015 Jul 7;132(1):27-39.
BACKGROUND: Patients with kidney disease have disordered bone and mineral metabolism, including elevated serum concentrations of fibroblast growth factor-23 (FGF23). These elevated concentrations are associated with cardiovascular and all-cause mortality. The objective was to determine the effects of the calcimimetic cinacalcet (versus placebo) on reducing serum FGF23 and whether changes in FGF23 are associated with death and cardiovascular events. METHODS AND RESULTS: This was a secondary analysis of a randomized clinical trial comparing cinacalcet to placebo in addition to conventional therapy (phosphate binders/vitamin D) in patients receiving hemodialysis with secondary hyperparathyroidism (intact parathyroid hormone >/=300 pg/mL). The primary study end point was time to death or a first nonfatal cardiovascular event (myocardial infarction, hospitalization for angina, heart failure, or a peripheral vascular event). This analysis included 2985 patients (77% of randomized) with serum samples at baseline and 2602 patients (67%) with samples at both baseline and week 20. The results demonstrated that a significantly larger proportion of patients randomized to cinacalcet had >/=30% (68% versus 28%) reductions in FGF23. Among patients randomized to cinacalcet, a >/=30% reduction in FGF23 between baseline and week 20 was associated with a nominally significant reduction in the primary composite end point (relative hazard, 0.82; 95% confidence interval, 0.69-0.98), cardiovascular mortality (relative hazard, 0.66; 95% confidence interval, 0.50-0.87), sudden cardiac death (relative hazard, 0.57; 95% confidence interval, 0.37-0.86), and heart failure (relative hazard, 0.69; 95% confidence interval, 0.48-0.99). CONCLUSIONS: Treatment with cinacalcet significantly lowers serum FGF23. Treatment-induced reductions in serum FGF23 are associated with lower rates of cardiovascular death and major cardiovascular events. CLINICAL TRIAL REGISTRATION: URL: http://www.clinicaltrials.gov. Unique identifier: NCT00345839.
Effects of cinacalcet on atherosclerotic and nonatherosclerotic cardiovascular events in patients receiving hemodialysis: the EValuation Of Cinacalcet HCl Therapy to Lower CardioVascular Events (EVOLVE) trial.[Pubmed:25404192]
J Am Heart Assoc. 2014 Nov 17;3(6):e001363.
BACKGROUND: Premature cardiovascular disease limits the duration and quality of life on long-term hemodialysis. The objective of this study was to define the frequency of fatal and nonfatal cardiovascular events attributable to atherosclerotic and nonatherosclerotic mechanisms, risk factors for these events, and the effects of cinacalcet, using adjudicated data collected during the EValuation of Cinacalcet HCl Therapy to Lower CardioVascular Events (EVOLVE) Trial. METHODS AND RESULTS: EVOLVE was a randomized, double-blind, placebo-controlled clinical trial that randomized 3883 hemodialysis patients with moderate to severe secondary hyperparathyroidism to cinacalcet or matched placebo for up to 64 months. For this post hoc analysis, the outcome measure was fatal and nonfatal cardiovascular events reflecting atherosclerotic and nonatherosclerotic cardiovascular diseases. During the trial, 1518 patients experienced an adjudicated cardiovascular event, including 958 attributable to nonatherosclerotic disease. Of 1421 deaths during the trial, 768 (54%) were due to cardiovascular disease. Sudden death was the most frequent fatal cardiovascular event, accounting for 24.5% of overall mortality. Combining fatal and nonfatal cardiovascular events, randomization to cinacalcet reduced the rates of sudden death and heart failure. Patients randomized to cinacalcet experienced fewer nonatherosclerotic cardiovascular events (adjusted relative hazard 0.84, 95% CI 0.74 to 0.96), while the effect of cinacalcet on atherosclerotic events did not reach statistical significance. CONCLUSIONS: Accepting the limitations of post hoc analysis, any benefits of cinacalcet on cardiovascular disease in the context of hemodialysis may result from attenuation of nonatherosclerotic processes. CLINICAL TRIALS REGISTRATION: Unique identifier: NCT00345839. URL: ClinicalTrials.gov.
