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作靶點(diǎn): CaSR作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (279.79 mM)* means s

2、oluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)

3、配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.69 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.69 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedCh

4、emE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.69 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Cinacalcet (AMG 073)種可服的 Ca receptor (CaR) 激動(dòng)劑，于治療管疾病。體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師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