Cinacalcet-AMG-073-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECinacalcetCat. No.: HY-70037CAS No.: 226256-56-0Synonyms: AMG 073分式: CHFN分量: 357.41作靶点: CaSR作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (279.79 mM)* means s

2、oluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7979 mL 13.9895 mL 27.9791 mL5 mM 0.5596 mL 2.7979 mL 5.5958 mL10 mM 0.2798 mL 1.3990 mL 2.7979 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现

3、配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.69 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.69 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedCh

4、emE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.69 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Cinacalcet (AMG 073)种可服的 Ca receptor (CaR) 激动剂，于治疗管疾病。体内研究 Cinacalcet HCl (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6nephrectomy animals. In sham an

5、imals, Cinacalcet HCl has no effect on parathyroid gland cell proliferationor parathyroid weight compared with vehicle treatment. There are no differences in serum phosphorus levelsin Cinacalcet HCl (10, 5, or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6nephrectomize

6、d animals. Cinacalcet HCl treatment significantly reduces blood ionized calcium levels in shamanimals 1. Cinacalcet (30 mg/kg/24 h) leads to a marked reduction in circulating parathyroid hormone and amodest reduction in serum Ca. Cinacalcet does not alter UCa when the GHS rats are fed the normal Ca

7、dietbut lowers UCa when they are fed the low Ca diet. Cinacalcet does not alter U supersaturation with respectto either CaOx or CaHPO4 on either diet 2.PROTOCOLAnimal To identify apoptosis in parathyroid glands from 5/6 nephrectomized or sham rats treated with vehicleAdministration 1 phosphate-buffe

8、red saline (PBS) or cinacalcet HCl (10 mg/kg), nuclear DNA fragmentation is measured insitu using the Apoptag System. Briefly, parathyroid gland sections from animals treated with vehicle orcinacalcet HCl are digested with 20 g/mL proteinase K in 0.1 mol/L PBS at room temperature for 15 minutesand i

9、ncubated with 3% hydrogen peroxide/methanol for 5 minutes to block endogenous peroxidase. Sectionsare incubated for 1 hour at 37C with terminal deoxynucleotidyl transferase (TdT) to label exposed 3-OHDNA ends with digoxigenin-tagged nucleotides. Digoxigenin-labeled DNA is detected by theimmunoperoxi

10、dase method. Sections are developed with 3,3-diaminobenzidine (DAB), and the nuclei ofapoptotic cells are stained brown. The specificity for apoptosis is verified by negative staining when distilledwater is substituted for TdT.MCE has not independently confirmed the accuracy of these methods. They a

11、re for reference only.户使本产品发表的科研献 J Med Chem. 2015 Apr 9;58(7):2958-66. Oxid Med Cell Longev. 2017;2017:3869561. J Biol Chem. 2016 Oct 28;291(44):23126-23135. Gen Comp Endocrinol. 2018 Oct 1;267:1-8. J Food Sci. 2018 Sep;83(9):2394-2401.See more customer validations on HYPERLINK / www.MedChemEREFERE

12、NCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Colloton M, et al. Cinacalcet HCl attenuates parathyroid hyperplasia in a rat model of secondary hyperparathyroidism. Kidney Int. 2005Feb;67(2):467-76.2. D.A. Bushinsky, et al. Effect of cinacalcet on urine calcium excretion and supersaturation in genetic hypercalciuric stone-forming rats.Kidney Int. 2006 May;69(9):1586-92.McePdfHeightCautio